Diazepam (T3D2903)

General Function:

Gaba-gated chloride ion channel activity

Specific Function:

Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel.

Gene Name:

GABRB3

Uniprot ID:

P28472

Molecular Weight:

54115.04 Da

References

1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [11752090 ]
2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [18384456 ]
3. Bagal SK, Brown AD, Cox PJ, Omoto K, Owen RM, Pryde DC, Sidders B, Skerratt SE, Stevens EB, Storer RI, Swain NA: Ion channels as therapeutic targets: a drug discovery perspective. J Med Chem. 2013 Feb 14;56(3):593-624. doi: 10.1021/jm3011433. Epub 2012 Nov 29. [23121096 ]
4. Huang Q, He X, Ma C, Liu R, Yu S, Dayer CA, Wenger GR, McKernan R, Cook JM: Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach. J Med Chem. 2000 Jan 13;43(1):71-95. [10633039 ]
5. Carling RW, Moore KW, Street LJ, Wild D, Isted C, Leeson PD, Thomas S, O'Connor D, McKernan RM, Quirk K, Cook SM, Atack JR, Wafford KA, Thompson SA, Dawson GR, Ferris P, Castro JL: 3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1. J Med Chem. 2004 Mar 25;47(7):1807-22. [15027873 ]
6. Russell MG, Carling RW, Atack JR, Bromidge FA, Cook SM, Hunt P, Isted C, Lucas M, McKernan RM, Mitchinson A, Moore KW, Narquizian R, Macaulay AJ, Thomas D, Thompson SA, Wafford KA, Castro JL: Discovery of functionally selective 7,8,9,10-tetrahydro-7,10-ethano-1,2,4-triazolo[3,4-a]phthalazines as GABA A receptor agonists at the alpha3 subunit. J Med Chem. 2005 Mar 10;48(5):1367-83. [15743180 ]
7. Goodacre SC, Street LJ, Hallett DJ, Crawforth JM, Kelly S, Owens AP, Blackaby WP, Lewis RT, Stanley J, Smith AJ, Ferris P, Sohal B, Cook SM, Pike A, Brown N, Wafford KA, Marshall G, Castro JL, Atack JR: Imidazo[1,2-a]pyrimidines as functionally selective and orally bioavailable GABA(A)alpha2/alpha3 binding site agonists for the treatment of anxiety disorders. J Med Chem. 2006 Jan 12;49(1):35-8. [16392789 ]
8. Street LJ, Sternfeld F, Jelley RA, Reeve AJ, Carling RW, Moore KW, McKernan RM, Sohal B, Cook S, Pike A, Dawson GR, Bromidge FA, Wafford KA, Seabrook GR, Thompson SA, Marshall G, Pillai GV, Castro JL, Atack JR, MacLeod AM: Synthesis and biological evaluation of 3-heterocyclyl-7,8,9,10-tetrahydro-(7,10-ethano)-1,2,4-triazolo[3,4-a]phthalazine s and analogues as subtype-selective inverse agonists for the GABA(A)alpha5 benzodiazepine binding site. J Med Chem. 2004 Jul 1;47(14):3642-57. [15214791 ]
9. Russell MG, Carling RW, Street LJ, Hallett DJ, Goodacre S, Mezzogori E, Reader M, Cook SM, Bromidge FA, Newman R, Smith AJ, Wafford KA, Marshall GR, Reynolds DS, Dias R, Ferris P, Stanley J, Lincoln R, Tye SJ, Sheppard WF, Sohal B, Pike A, Dominguez M, Atack JR, Castro JL: Discovery of imidazo[1,2-b][1,2,4]triazines as GABA(A) alpha2/3 subtype selective agonists for the treatment of anxiety. J Med Chem. 2006 Feb 23;49(4):1235-8. [16480260 ]
10. Carling RW, Madin A, Guiblin A, Russell MG, Moore KW, Mitchinson A, Sohal B, Pike A, Cook SM, Ragan IC, McKernan RM, Quirk K, Ferris P, Marshall G, Thompson SA, Wafford KA, Dawson GR, Atack JR, Harrison T, Castro JL, Street LJ: 7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl) -1,2,4-triazolo[4,3-b]pyridazine: a functionally selective gamma-aminobutyric acid(A) (GABA(A)) alpha2/alpha3-subtype selective agonist that exhibits potent anxiolytic activity but is not sedating in animal models. J Med Chem. 2005 Nov 17;48(23):7089-92. [16279764 ]
11. Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. [6738302 ]
12. Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. [2867566 ]

General Function:

Inhibitory extracellular ligand-gated ion channel activity

Specific Function:

GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.

Gene Name:

GABRA2

Uniprot ID:

P47869

Molecular Weight:

51325.85 Da

References

1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [11752352 ]
2. Collins I, Davey WB, Rowley M, Quirk K, Bromidge FA, McKernan RM, Thompson SA, Wafford KA: N-(indol-3-ylglyoxylyl)piperidines: high affinity agonists of human GABA-A receptors containing the alpha1 subunit. Bioorg Med Chem Lett. 2000 Jun 19;10(12):1381-4. [10890169 ]
3. Russell MG, Carling RW, Atack JR, Bromidge FA, Cook SM, Hunt P, Isted C, Lucas M, McKernan RM, Mitchinson A, Moore KW, Narquizian R, Macaulay AJ, Thomas D, Thompson SA, Wafford KA, Castro JL: Discovery of functionally selective 7,8,9,10-tetrahydro-7,10-ethano-1,2,4-triazolo[3,4-a]phthalazines as GABA A receptor agonists at the alpha3 subunit. J Med Chem. 2005 Mar 10;48(5):1367-83. [15743180 ]
4. Goodacre SC, Street LJ, Hallett DJ, Crawforth JM, Kelly S, Owens AP, Blackaby WP, Lewis RT, Stanley J, Smith AJ, Ferris P, Sohal B, Cook SM, Pike A, Brown N, Wafford KA, Marshall G, Castro JL, Atack JR: Imidazo[1,2-a]pyrimidines as functionally selective and orally bioavailable GABA(A)alpha2/alpha3 binding site agonists for the treatment of anxiety disorders. J Med Chem. 2006 Jan 12;49(1):35-8. [16392789 ]
5. Huang Q, He X, Ma C, Liu R, Yu S, Dayer CA, Wenger GR, McKernan R, Cook JM: Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach. J Med Chem. 2000 Jan 13;43(1):71-95. [10633039 ]
6. Carling RW, Moore KW, Street LJ, Wild D, Isted C, Leeson PD, Thomas S, O'Connor D, McKernan RM, Quirk K, Cook SM, Atack JR, Wafford KA, Thompson SA, Dawson GR, Ferris P, Castro JL: 3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1. J Med Chem. 2004 Mar 25;47(7):1807-22. [15027873 ]
7. Carling RW, Madin A, Guiblin A, Russell MG, Moore KW, Mitchinson A, Sohal B, Pike A, Cook SM, Ragan IC, McKernan RM, Quirk K, Ferris P, Marshall G, Thompson SA, Wafford KA, Dawson GR, Atack JR, Harrison T, Castro JL, Street LJ: 7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl) -1,2,4-triazolo[4,3-b]pyridazine: a functionally selective gamma-aminobutyric acid(A) (GABA(A)) alpha2/alpha3-subtype selective agonist that exhibits potent anxiolytic activity but is not sedating in animal models. J Med Chem. 2005 Nov 17;48(23):7089-92. [16279764 ]
8. Street LJ, Sternfeld F, Jelley RA, Reeve AJ, Carling RW, Moore KW, McKernan RM, Sohal B, Cook S, Pike A, Dawson GR, Bromidge FA, Wafford KA, Seabrook GR, Thompson SA, Marshall G, Pillai GV, Castro JL, Atack JR, MacLeod AM: Synthesis and biological evaluation of 3-heterocyclyl-7,8,9,10-tetrahydro-(7,10-ethano)-1,2,4-triazolo[3,4-a]phthalazine s and analogues as subtype-selective inverse agonists for the GABA(A)alpha5 benzodiazepine binding site. J Med Chem. 2004 Jul 1;47(14):3642-57. [15214791 ]
9. Russell MG, Carling RW, Street LJ, Hallett DJ, Goodacre S, Mezzogori E, Reader M, Cook SM, Bromidge FA, Newman R, Smith AJ, Wafford KA, Marshall GR, Reynolds DS, Dias R, Ferris P, Stanley J, Lincoln R, Tye SJ, Sheppard WF, Sohal B, Pike A, Dominguez M, Atack JR, Castro JL: Discovery of imidazo[1,2-b][1,2,4]triazines as GABA(A) alpha2/3 subtype selective agonists for the treatment of anxiety. J Med Chem. 2006 Feb 23;49(4):1235-8. [16480260 ]
10. Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. [6738302 ]
11. Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. [2867566 ]

General Function:

Inhibitory extracellular ligand-gated ion channel activity

Specific Function:

GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.

Gene Name:

GABRA3

Uniprot ID:

P34903

Molecular Weight:

55164.055 Da

References

1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [11752352 ]
2. Jacobsen EJ, TenBrink RE, Stelzer LS, Belonga KL, Carter DB, Im HK, Im WB, Sethy VH, Tang AH, VonVoigtlander PF, Petke JD: High-affinity partial agonist imidazo[1,5-a]quinoxaline amides, carbamates, and ureas at the gamma-aminobutyric acid A/benzodiazepine receptor complex. J Med Chem. 1996 Jan 5;39(1):158-75. [8568803 ]
3. Lager E, Andersson P, Nilsson J, Pettersson I, Nielsen EO, Nielsen M, Sterner O, Liljefors T: 4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling. J Med Chem. 2006 Apr 20;49(8):2526-33. [16610795 ]
4. Carling RW, Moore KW, Street LJ, Wild D, Isted C, Leeson PD, Thomas S, O'Connor D, McKernan RM, Quirk K, Cook SM, Atack JR, Wafford KA, Thompson SA, Dawson GR, Ferris P, Castro JL: 3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1. J Med Chem. 2004 Mar 25;47(7):1807-22. [15027873 ]
5. Carling RW, Madin A, Guiblin A, Russell MG, Moore KW, Mitchinson A, Sohal B, Pike A, Cook SM, Ragan IC, McKernan RM, Quirk K, Ferris P, Marshall G, Thompson SA, Wafford KA, Dawson GR, Atack JR, Harrison T, Castro JL, Street LJ: 7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl) -1,2,4-triazolo[4,3-b]pyridazine: a functionally selective gamma-aminobutyric acid(A) (GABA(A)) alpha2/alpha3-subtype selective agonist that exhibits potent anxiolytic activity but is not sedating in animal models. J Med Chem. 2005 Nov 17;48(23):7089-92. [16279764 ]
6. Street LJ, Sternfeld F, Jelley RA, Reeve AJ, Carling RW, Moore KW, McKernan RM, Sohal B, Cook S, Pike A, Dawson GR, Bromidge FA, Wafford KA, Seabrook GR, Thompson SA, Marshall G, Pillai GV, Castro JL, Atack JR, MacLeod AM: Synthesis and biological evaluation of 3-heterocyclyl-7,8,9,10-tetrahydro-(7,10-ethano)-1,2,4-triazolo[3,4-a]phthalazine s and analogues as subtype-selective inverse agonists for the GABA(A)alpha5 benzodiazepine binding site. J Med Chem. 2004 Jul 1;47(14):3642-57. [15214791 ]
7. Collins I, Davey WB, Rowley M, Quirk K, Bromidge FA, McKernan RM, Thompson SA, Wafford KA: N-(indol-3-ylglyoxylyl)piperidines: high affinity agonists of human GABA-A receptors containing the alpha1 subunit. Bioorg Med Chem Lett. 2000 Jun 19;10(12):1381-4. [10890169 ]
8. Russell MG, Carling RW, Atack JR, Bromidge FA, Cook SM, Hunt P, Isted C, Lucas M, McKernan RM, Mitchinson A, Moore KW, Narquizian R, Macaulay AJ, Thomas D, Thompson SA, Wafford KA, Castro JL: Discovery of functionally selective 7,8,9,10-tetrahydro-7,10-ethano-1,2,4-triazolo[3,4-a]phthalazines as GABA A receptor agonists at the alpha3 subunit. J Med Chem. 2005 Mar 10;48(5):1367-83. [15743180 ]
9. Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. [6738302 ]
10. Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. [2867566 ]

General Function:

Inhibitory extracellular ligand-gated ion channel activity

Specific Function:

Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel (By similarity).

Gene Name:

GABRA1

Uniprot ID:

P14867

Molecular Weight:

51801.395 Da

References

1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [17139284 ]
2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [17016423 ]
3. Harris D, Clayton T, Cook J, Sahbaie P, Halliwell RF, Furtmuller R, Huck S, Sieghart W, DeLorey TM: Selective influence on contextual memory: physiochemical properties associated with selectivity of benzodiazepine ligands at GABAA receptors containing the alpha5 subunit. J Med Chem. 2008 Jul 10;51(13):3788-803. doi: 10.1021/jm701433b. Epub 2008 Jun 7. [18537233 ]
4. Hadingham KL, Garrett EM, Wafford KA, Bain C, Heavens RP, Sirinathsinghji DJ, Whiting PJ: Cloning of cDNAs encoding the human gamma-aminobutyric acid type A receptor alpha 6 subunit and characterization of the pharmacology of alpha 6-containing receptors. Mol Pharmacol. 1996 Feb;49(2):253-9. [8632757 ]

General Function:

Cholesterol binding

Specific Function:

Can bind protoporphyrin IX and may play a role in the transport of porphyrins and heme (By similarity). Promotes the transport of cholesterol across mitochondrial membranes and may play a role in lipid metabolism (PubMed:24814875), but its precise physiological role is controversial. It is apparently not required for steroid hormone biosynthesis. Was initially identified as peripheral-type benzodiazepine receptor; can also bind isoquinoline carboxamides (PubMed:1847678).

Gene Name:

TSPO

Uniprot ID:

P30536

Molecular Weight:

18827.81 Da

References

1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [11752352 ]
2. Falchi AM, Battetta B, Sanna F, Piludu M, Sogos V, Serra M, Melis M, Putzolu M, Diaz G: Intracellular cholesterol changes induced by translocator protein (18 kDa) TSPO/PBR ligands. Neuropharmacology. 2007 Aug;53(2):318-29. Epub 2007 Jun 2. [17631921 ]
3. Han WQ, Wang LJ, Sun XY, Li JS: Treatment of bactericide wastewater by combined process chemical coagulation, electrochemical oxidation and membrane bioreactor. J Hazard Mater. 2008 Mar 1;151(2-3):306-15. Epub 2007 Jun 7. [17662522 ]
4. Chen Z, Kong X: Study of Candida albicans vaginitis model in Kunming mice. J Huazhong Univ Sci Technolog Med Sci. 2007 Jun;27(3):307-10. [17641849 ]
5. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [17139284 ]
6. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [17016423 ]

General Function:

Transporter activity

Specific Function:

GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.

Gene Name:

GABRA5

Uniprot ID:

P31644

Molecular Weight:

52145.645 Da

References

1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [11752090 ]
2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [18384456 ]
3. Derry JM, Dunn SM, Davies M: Identification of a residue in the gamma-aminobutyric acid type A receptor alpha subunit that differentially affects diazepam-sensitive and -insensitive benzodiazepine site binding. J Neurochem. 2004 Mar;88(6):1431-8. [15009644 ]
4. Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. [6738302 ]
5. Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. [2867566 ]

General Function:

Inhibitory extracellular ligand-gated ion channel activity

Specific Function:

GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.

Gene Name:

GABRA6

Uniprot ID:

Q16445

Molecular Weight:

51023.69 Da

References

1. Hadingham KL, Garrett EM, Wafford KA, Bain C, Heavens RP, Sirinathsinghji DJ, Whiting PJ: Cloning of cDNAs encoding the human gamma-aminobutyric acid type A receptor alpha 6 subunit and characterization of the pharmacology of alpha 6-containing receptors. Mol Pharmacol. 1996 Feb;49(2):253-9. [8632757 ]
2. TenBrink RE, Im WB, Sethy VH, Tang AH, Carter DB: Antagonist, partial agonist, and full agonist imidazo[1,5-a]quinoxaline amides and carbamates acting through the GABAA/benzodiazepine receptor. J Med Chem. 1994 Mar 18;37(6):758-68. [8145225 ]
3. Jacobsen EJ, TenBrink RE, Stelzer LS, Belonga KL, Carter DB, Im HK, Im WB, Sethy VH, Tang AH, VonVoigtlander PF, Petke JD: High-affinity partial agonist imidazo[1,5-a]quinoxaline amides, carbamates, and ureas at the gamma-aminobutyric acid A/benzodiazepine receptor complex. J Med Chem. 1996 Jan 5;39(1):158-75. [8568803 ]

General Function:

Ligand-gated ion channel activity

Specific Function:

Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel (By similarity).

Gene Name:

GABRB1

Uniprot ID:

P18505

Molecular Weight:

54234.085 Da

References

1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [11752090 ]
2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [18384456 ]
3. Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. [6738302 ]
4. Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. [2867566 ]

General Function:

Inhibitory extracellular ligand-gated ion channel activity

Specific Function:

Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel.

Gene Name:

GABRB2

Uniprot ID:

P47870

Molecular Weight:

59149.895 Da

References

1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [11752090 ]
2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [18384456 ]
3. Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. [6738302 ]
4. Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. [2867566 ]

General Function:

Gaba-a receptor activity

Specific Function:

GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.

Gene Name:

GABRD

Uniprot ID:

O14764

Molecular Weight:

50707.835 Da

References

1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [11752090 ]
2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [18384456 ]
3. Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. [6738302 ]
4. Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. [2867566 ]

General Function:

Inhibitory extracellular ligand-gated ion channel activity

Specific Function:

GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.

Gene Name:

GABRE

Uniprot ID:

P78334

Molecular Weight:

57971.175 Da

References

1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [11752090 ]
2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [18384456 ]
3. Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. [6738302 ]
4. Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. [2867566 ]

General Function:

Inhibitory extracellular ligand-gated ion channel activity

Specific Function:

GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.

Gene Name:

GABRG1

Uniprot ID:

Q8N1C3

Molecular Weight:

53594.49 Da

References

1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [11752090 ]
2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [18384456 ]
3. Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. [6738302 ]
4. Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. [2867566 ]

General Function:

Inhibitory extracellular ligand-gated ion channel activity

Specific Function:

Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel.

Gene Name:

GABRG2

Uniprot ID:

P18507

Molecular Weight:

54161.78 Da

References

1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [11752090 ]
2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [18384456 ]
3. Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. [6738302 ]
4. Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. [2867566 ]

General Function:

Inhibitory extracellular ligand-gated ion channel activity

Specific Function:

GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.

Gene Name:

GABRG3

Uniprot ID:

Q99928

Molecular Weight:

54288.16 Da

References

1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [11752090 ]
2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [18384456 ]
3. Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. [6738302 ]
4. Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. [2867566 ]

General Function:

Gaba-a receptor activity

Specific Function:

GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel. In the uterus, the function of the receptor appears to be related to tissue contractility. The binding of this pI subunit with other GABA(A) receptor subunits alters the sensitivity of recombinant receptors to modulatory agents such as pregnanolone.

Gene Name:

GABRP

Uniprot ID:

O00591

Molecular Weight:

50639.735 Da

References

1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [11752090 ]
2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [18384456 ]
3. Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. [6738302 ]
4. Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. [2867566 ]

General Function:

Gaba-a receptor activity

Specific Function:

GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel. Rho-1 GABA receptor could play a role in retinal neurotransmission.

Gene Name:

GABRR1

Uniprot ID:

P24046

Molecular Weight:

55882.91 Da

References

1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [11752090 ]
2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [18384456 ]
3. Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. [6738302 ]
4. Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. [2867566 ]

General Function:

Gaba-a receptor activity

Specific Function:

GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel. Rho-2 GABA receptor could play a role in retinal neurotransmission.

Gene Name:

GABRR2

Uniprot ID:

P28476

Molecular Weight:

54150.41 Da

References

1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [11752090 ]
2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [18384456 ]
3. Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. [6738302 ]
4. Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. [2867566 ]

General Function:

Gaba-a receptor activity

Specific Function:

GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.

Gene Name:

GABRR3

Uniprot ID:

A8MPY1

Molecular Weight:

54271.1 Da

References

1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [11752090 ]
2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [18384456 ]
3. Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. [6738302 ]
4. Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. [2867566 ]

General Function:

Transmembrane signaling receptor activity

Specific Function:

GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.

Gene Name:

GABRQ

Uniprot ID:

Q9UN88

Molecular Weight:

72020.875 Da

References

1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [11752090 ]
2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [18384456 ]

General Function:

G-protein coupled adenosine receptor activity

Specific Function:

Receptor for adenosine. The activity of this receptor is mediated by G proteins which inhibits adenylyl cyclase. Possible role in reproduction.

Gene Name:

ADORA3

Uniprot ID:

P0DMS8

Molecular Weight:

36184.175 Da

References

1. Minetti P, Tinti MO, Carminati P, Castorina M, Di Cesare MA, Di Serio S, Gallo G, Ghirardi O, Giorgi F, Giorgi L, Piersanti G, Bartoccini F, Tarzia G: 2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization. J Med Chem. 2005 Nov 3;48(22):6887-96. [16250647 ]

General Function:

Peptide binding

Specific Function:

Receptor for cholecystokinin. Mediates pancreatic growth and enzyme secretion, smooth muscle contraction of the gall bladder and stomach. Has a 1000-fold higher affinity for CCK rather than for gastrin. It modulates feeding and dopamine-induced behavior in the central and peripheral nervous system. This receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system.

Gene Name:

CCKAR

Uniprot ID:

P32238

Molecular Weight:

47840.645 Da

References

1. Evans BE, Rittle KE, Bock MG, DiPardo RM, Freidinger RM, Whitter WL, Gould NP, Lundell GF, Homnick CF, Veber DF, et al.: Design of nonpeptidal ligands for a peptide receptor: cholecystokinin antagonists. J Med Chem. 1987 Jul;30(7):1229-39. [2885419 ]

General Function:

Not Available

Specific Function:

Keratin-binding protein required for epithelial cell polarization. Involved in apical junction complex (AJC) assembly via its interaction with PARD3. Required for ciliogenesis.

Gene Name:

FBF1

Uniprot ID:

Q8TES7

Molecular Weight:

125445.19 Da

References

1. Yoo MJ, Hage DS: Use of peak decay analysis and affinity microcolumns containing silica monoliths for rapid determination of drug-protein dissociation rates. J Chromatogr A. 2011 Apr 15;1218(15):2072-8. doi: 10.1016/j.chroma.2010.09.070. Epub 2010 Oct 16. [20956006 ]

General Function:

Toxic substance binding

Specific Function:

Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloidal osmotic pressure of blood. Major zinc transporter in plasma, typically binds about 80% of all plasma zinc.

Gene Name:

ALB

Uniprot ID:

P02768

Molecular Weight:

69365.94 Da

References

1. Lazaro E, Lowe PJ, Briand X, Faller B: New approach to measure protein binding based on a parallel artificial membrane assay and human serum albumin. J Med Chem. 2008 Apr 10;51(7):2009-17. doi: 10.1021/jm7012826. Epub 2008 Mar 19. [18348514 ]

General Function:

Inhibitory extracellular ligand-gated ion channel activity

Specific Function:

Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel (By similarity).

Included Proteins:

P14867 , P47869 , P34903 , P48169 , P31644 , Q16445 , P18505 , P47870 , P28472 , O14764 , P78334 , Q8N1C3 , P18507 , Q99928 , O00591 , Q9UN88