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Target 1
[top]
|
| Target 1 ID |
1143 |
| Target 1 Name |
Alpha-2A adrenergic receptor |
| Target 1 Mechanism of Action |
Brimonidine is an alpha adrenergic receptor agonist. It has a peak ocular hypotensive effect occurring at two hours post-dosing. Fluorophotometric studies in animals and humans suggest that Brimonidine has a dual mechanism of action by reducing aqueous humor production and increasing uveoscleral outflow. |
| Target 1 Description |
Alpha-2 adrenergic receptors mediate the catecholamine- induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazoline > clonidine > epinephrine > norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p-octopamine. For antagonists, the rank order is yohimbine > phentolamine = mianserine > chlorpromazine = spiperone = prazosin > propanolol > alprenolol = pindolol |
| Target 1 Synonyms |
- Alpha-2A adrenoreceptor; Alpha-2A adrenoceptor; Alpha-2AAR; Alpha-2 adrenergic receptor subtype C10
|
| Target 1 Gene Name |
ADRA2A |
| Target 1 Protein Sequence |
>Alpha-2A adrenergic receptor
MGSLQPDAGNASWNGTEAPGGGARATPYSLQVTLTLVCLAGLLMLLTVFGNVLVIIAVFT
SRALKAPQNLFLVSLASADILVATLVIPFSLANEVMGYWYFGKAWCEIYLALDVLFCTSS
IVHLCAISLDRYWSITQAIEYNLKRTPRRIKAIIITVWVISAVISFPPLISIEKKGGGGG
PQPAEPRCEINDQKWYVISSCIGSFFAPCLIMILVYVRIYQIAKRRTRVPPSRRGPDAVA
APPGGTERRPNGLGPERSAGPGGAEAEPLPTQLNGAPGEPAPAGPRDTDALDLEESSSSD
HAERPPGPRRPERGPRGKGKARASQVKPGDSLPRRGPGATGIGTPAAGPGEERVGAAKAS
RWRGRQNREKRFTFVLAVVIGVFVVCWFPFFFTYTLTAVGCSVPRTLFKFFFWFGYCNSS
LNPVIYTIFNHDFRRAFKKILCRGDRKRIV
|
| Target 1 Number of Residues |
450 |
| Target 1 Molecular Weight |
48956.3 |
| Target 1 Theoretical pI |
10.20 |
| Target 1 GO Classification |
|
Function
|
amine receptor activity
adrenoceptor activity
alpha-adrenergic receptor activity
alpha2-adrenergic receptor activity
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity |
|
Process
|
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway |
|
Component
|
cell
membrane
intrinsic to membrane
integral to membrane |
|
| Target 1 General Function |
Involved in alpha2-adrenergic receptor activity |
| Target 1 Pathways |
Not Available |
| Target 1 Reactions |
Not Available |
| Target 1 Signals |
|
| Target 1 Transmembrane Regions |
- 34-59
- 71-96
- 107-129
- 152-172
- 195-217
- 375-395
- 410-429
|
| Target 1 Essentiality |
Non Essential |
| Target 1 Domain Function |
PF00001:7tm_1 |
| Target 1 GenBank ID Protein |
Not Available |
| Target 1 UniProtKB ID |
P08913  |
| Target 1 Cellular Location |
Cell membrane |
| Target 1 Gene Sequence |
>1353 bp
ATGGGCTCCCTGCAGCCGGACGCGGGCAACGCGAGCTGGAACGGGACCGAGGCGCCGGGG
GGCGGCGCCCGGGCCACCCCTTACTCCCTGCAGGTGACGCTGACGCTGGTGTGCCTGGCC
GGCCTGCTCATGCTGCTCACCGTGTTCGGCAACGTGCTCGTCATCATCGCCGTGTTCACG
AGCCGCGCGCTCAAGGCGCCCCAAAACCTCTTCCTGGTGTCTCTGGCCTCGGCCGACATC
CTGGTGGCCACGCTCGTCATCCCTTTCTCGCTGGCCAACGAGGTCATGGGCTACTGGTAC
TTCGGCAAGGCTTGGTGCGAGATCTACCTGGCGCTCGACGTGCTCTTCTGCACGTCGTCC
ATCGTGCACCTGTGCGCCATCAGCCTGGACCGCTACTGGTCCATCACACAGGCCATCGAG
TACAACCTGAAGCGCACGCCGCGCCGCATCAAGGCCATCATCATCACCGTGTGGGTCATC
TCGGCCGTCATCTCCTTCCCGCCGCTCATCTCCATCGAGAAGAAGGGCGGCGGCGGCGGC
CCGCAGCCGGCCGAGCCGCGCTGCGAGATCAACGACCAGAAGTGGTACGTCATCTCGTCG
TGCATCGGCTCCTTCTTCGCTCCCTGCCTCATCATGATCCTGGTCTACGTGCGCATCTAC
CAGATCGCCAAGCGTCGCACCCGCGTGCCACCCAGCCGCCGGGGTCCGGACGCCGTCGCC
GCGCCGCCGGGGGGCACCGAGCGCAGGCCCAACGGTCTGGGCCCCGAGCGCAGCGCGGGC
CCGGGGGGCGCAGAGGCCGAACCGCTGCCCACCCAGCTCAACGGCGCCCCTGGCGAGCCC
GCGCCGGCCGGGCCGCGCGACACCGACGCGCTGGACCTGGAGGAGAGCTCGTCTTCCGAC
CACGCCGAGCGGCCTCCAGGGCCCCGCAGACCCGAGCGCGGTCCCCGGGGCAAAGGCAAG
GCCCGAGCGAGCCAGGTGAAGCCGGGCGACAGCCTGCCGCGGCGCGGGCCGGGGGCGACG
GGGATCGGGACGCCGGCTGCAGGGCCGGGGGAGGAGCGCGTCGGGGCTGCCAAGGCGTCG
CGCTGGCGCGGGCGGCAGAACCGCGAGAAGCGCTTCACGTTCGTGCTGGCCGTGGTCATC
GGAGTGTTCGTGGTGTGCTGGTTCCCCTTCTTCTTCACCTACACGCTCACGGCCGTCGGG
TGCTCCGTGCCACGCACGCTCTTCAAATTCTTCTTCTGGTTCGGCTACTGCAACAGCTCG
TTGAACCCGGTCATCTACACCATCTTCAACCACGATTTCCGCCGCGCCTTCAAGAAGATC
CTCTGTCGGGGGGACAGGAAGCGGATCGTGTGA
|
| Target 1 GenBank Gene ID |
Not Available |
| Target 1 GeneCard ID |
ADRA2A |
| Target 1 GenAtlas ID |
ADRA2A |
| Target 1 HGNC ID |
HGNC:281 |
| Target 1 Chromosome Location |
Chromosome:10 |
| Target 1 Locus |
10q24-q26 |
| Target 1 SNPs |
SNPJam Report |
| Target 1 Toxin References |
- V514 - Rauly I, Ailhaud M, Wurch T, Pauwels PJ: alpha(2A)-adrenoceptor: G(alphai1) protein-mediated pertussis toxin-resistant attenuation of G(s) coupling to the cyclic AMP pathway. Biochem Pharmacol. 2000 Jun 15;59(12):1531-8. [PubMed ]
- V515 - Wikberg-Matsson A, Simonsen U: Potent alpha(2A)-adrenoceptor-mediated vasoconstriction by brimonidine in porcine ciliary arteries. Invest Ophthalmol Vis Sci. 2001 Aug;42(9):2049-55. [PubMed ]
- V516 - Meana JJ, Barturen F, Garro MA, Garcia-Sevilla JA, Fontan A, Zarranz JJ: Decreased density of presynaptic alpha 2-adrenoceptors in postmortem brains of patients with Alzheimer's disease. J Neurochem. 1992 May;58(5):1896-904. [PubMed ]
|
| Target 1 General References |
2823383; 2568356; 2170371; 10948191; 16567612 |
|
Target 2
[top]
|
| Target 2 ID |
1240 |
| Target 2 Name |
Alpha-2B adrenergic receptor |
| Target 2 Mechanism of Action |
Brimonidine is an alpha adrenergic receptor agonist. It has a peak ocular hypotensive effect occurring at two hours post-dosing. Fluorophotometric studies in animals and humans suggest that Brimonidine has a dual mechanism of action by reducing aqueous humor production and increasing uveoscleral outflow. |
| Target 2 Description |
Alpha-2 adrenergic receptors mediate the catecholamine- induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is clonidine > norepinephrine > epinephrine = oxymetazoline > dopamine > p-tyramine = phenylephrine > serotonin > p-synephrine / p-octopamine. For antagonists, the rank order is yohimbine > chlorpromazine > phentolamine > mianserine > spiperone > prazosin > alprenolol > propanolol > pindolol |
| Target 2 Synonyms |
- Alpha-2B adrenoreceptor; Alpha-2B adrenoceptor; Alpha-2 adrenergic receptor subtype C2
|
| Target 2 Gene Name |
ADRA2B |
| Target 2 Protein Sequence |
>Alpha-2B adrenergic receptor
MDHQDPYSVQATAAIAAAITFLILFTIFGNALVILAVLTSRSLRAPQNLFLVSLAAADIL
VATLIIPFSLANELLGYWYFRRTWCEVYLALDVLFCTSSIVHLCAISLDRYWAVSRALEY
NSKRTPRRIKCIILTVWLIAAVISLPPLIYKGDQGPQPRGRPQCKLNQEAWYILASSIGS
FFAPCLIMILVYLRIYLIAKRSNRRGPRAKGGPGQGESKQPRPDHGGALASAKLPALASV
ASAREVNGHSKSTGEKEEGETPEDTGTRALPPSWAALPNSGQGQKEGVCGASPEDEAEEE
EEEEEEEEECEPQAVPVSPASACSPPLQQPQGSRVLATLRGQVLLGRGVGAIGGQWWRRR
AQLTREKRFTFVLAVVIGVFVLCWFPFFFSYSLGAICPKHCKVPHGLFQFFFWIGYCNSS
LNPVIYTIFNQDFRRAFRRILCRPWTQTAW
|
| Target 2 Number of Residues |
450 |
| Target 2 Molecular Weight |
49953.1 |
| Target 2 Theoretical pI |
8.52 |
| Target 2 GO Classification |
|
Function
|
amine receptor activity
adrenoceptor activity
alpha-adrenergic receptor activity
alpha2-adrenergic receptor activity
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity |
|
Process
|
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway |
|
Component
|
cell
membrane
intrinsic to membrane
integral to membrane |
|
| Target 2 General Function |
Involved in alpha2-adrenergic receptor activity |
| Target 2 Pathways |
Not Available |
| Target 2 Reactions |
Not Available |
| Target 2 Signals |
|
| Target 2 Transmembrane Regions |
- 13-38
- 50-75
- 86-108
- 131-153
- 170-193
- 373-396
- 406-429
|
| Target 2 Essentiality |
Non Essential |
| Target 2 Domain Function |
PF00001:7tm_1 |
| Target 2 GenBank ID Protein |
Not Available |
| Target 2 UniProtKB ID |
P18089 |
| Target 2 Cellular Location |
Cell membrane |
| Target 2 Gene Sequence |
>1353 bp
CCCGCCCCGTCATGGACCACCAGGACCCCTACTCCGTGCAGGCCACAGCGGCCATAGCGG
CGGCCATCACCTTCCTCATTCTCTTTACCATCTTCGGCAACGCTCTGGTCATCCTGGCTG
TGTTGACCAGCCGCTCGCTGCGCGCCCCTCAGAACCTGTTCCTGGTGTCGCTGGCCGCCG
CCGACATCCTGGTGGCCACGCTCATCATCCCTTTCTCGCTGGCCAACGAGCTGCTGGGCT
ACTGGTACTTCCGGCGCACGTGGTGCGAGGTGTACCTGGCGCTCGACGTGCTCTTCTGCA
CCTCGTCCATCGTGCACCTGTGCGCCATCAGCCTGGACCGCTACTGGGCCGTGAGCCGCG
CGCTGGAGTACAACTCCAAGCGCACCCCGCGCCGCATCAAGTGCATCATCCTCACTGTGT
GGCTCATCGCCGCCGTCATCTCGCTGCCGCCCCTCATCTACAAGGGCGACCAGGGCCCCC
AGCCGCGCGGGCGCCCCCAGTGCAAGCTCAACCAGGAGGCCTGGTACATCCTGGCCTCCA
GCATCGGATCTTTCTTTGCTCCTTGCCTCATCATGATCCTTGTCTACCTGCGCATCTACC
TGATCGCCAAACGCAGCAACCGCAGAGGTCCCAGGGCCAAGGGGGGGCCTGGGCAGGGTG
AGTCCAAGCAGCCCCGACCCGACCATGGTGGGGCTTTGGCCTCAGCCAAACTGCCAGCCC
TGGCCTCTGTGGCTTCTGCCAGAGAGGTCAACGGACACTCGAAGTCCACTGGGGAGAAGG
AGGAGGGGGAGACCCCTGAAGATACTGGGACCCGGGCCTTGCCACCCAGTTGGGCTGCCC
TTCCCAACTCAGGCCAGGGCCAGAAGGAGGGTGTTTGTGGGGCATCTCCAGAGGATGAAG
CTGAAGAGGAGGAAGAGGAGGAGGAGGAGGAGGAAGAGTGTGAACCCCAGGCAGTGCCAG
TGTCTCCGGCCTCAGCTTGCAGCCCCCCGCTGCAGCAGCCACAGGGCTCCCGGGTGCTGG
CCACCCTACGTGGCCAGGTGCTCCTGGGCAGGGGCGTGGGTGCTATAGGTGGGCAGTGGT
GGCGTCGAAGGGCGCACGTGACCCGGGAGAAGCGCTTCACCTTCGTGCTGGCTGTGGTCA
TTGGCGTTTTTGTGCTCTGCTGGTTCCCCTTCTTCTTCAGCTACAGCCTGGGCGCCATCT
GCCCGAAGCACTGCAAGGTGCCCCATGGCCTCTTCCAGTTCTTCTTCTGGATCGGCTACT
GCAACAGCTCACTGAACCCTGTTATCTACACCATCTTCAACCAGGACTTCCGCCGTGCCT
TCCGGAGGATCCTGTGCCGCCCGTGGACCCAGA
|
| Target 2 GenBank Gene ID |
Not Available |
| Target 2 GeneCard ID |
ADRA2B |
| Target 2 GenAtlas ID |
ADRA2B |
| Target 2 HGNC ID |
HGNC:282 |
| Target 2 Chromosome Location |
Not Available |
| Target 2 Locus |
2p13-q13 |
| Target 2 SNPs |
SNPJam Report |
| Target 2 Toxin References |
- V517 - Trendelenburg AU, Philipp M, Meyer A, Klebroff W, Hein L, Starke K: All three alpha2-adrenoceptor types serve as autoreceptors in postganglionic sympathetic neurons. Naunyn Schmiedebergs Arch Pharmacol. 2003 Dec;368(6):504-12. Epub 2003 Nov 11. [PubMed ]
- V518 - Bohmann C, Schollmeyer P, Rump LC: Methoxamine inhibits noradrenaline release through activation of alpha 1- and alpha 2-adrenoceptors in rat isolated kidney: involvement of purines and prostaglandins. Naunyn Schmiedebergs Arch Pharmacol. 1993 Mar;347(3):273-9. [PubMed ]
|
| Target 2 General References |
2164221; 2172775; 11056163; 15037199; 15815621; 2173582 |
|
Target 3
[top]
|
| Target 3 ID |
1367 |
| Target 3 Name |
Alpha-2C adrenergic receptor |
| Target 3 Mechanism of Action |
Brimonidine is an alpha adrenergic receptor agonist. It has a peak ocular hypotensive effect occurring at two hours post-dosing. Fluorophotometric studies in animals and humans suggest that Brimonidine has a dual mechanism of action by reducing aqueous humor production and increasing uveoscleral outflow. |
| Target 3 Description |
Alpha-2 adrenergic receptors mediate the catecholamine- induced inhibition of adenylate cyclase through the action of G proteins |
| Target 3 Synonyms |
- Alpha-2C adrenoreceptor; Alpha-2C adrenoceptor; Alpha-2 adrenergic receptor subtype C4
|
| Target 3 Gene Name |
ADRA2C |
| Target 3 Protein Sequence |
>Alpha-2C adrenergic receptor
MASPALAAALAVAAAAGPNASGAGERGSGGVANASGASWGPPRGQYSAGAVAGLAAVVGF
LIVFTVVGNVLVVIAVLTSRALRAPQNLFLVSLASADILVATLVMPFSLANELMAYWYFG
QVWCGVYLALDVLFCTSSIVHLCAISLDRYWSVTQAVEYNLKRTPRRVKATIVAVWLISA
VISFPPLVSLYRQPDGAAYPQCGLNDETWYILSSCIGSFFAPCLIMGLVYARIYRVAKLR
TRTLSEKRAPVGPDGASPTTENGLGAAAGAGENGHCAPPPADVEPDESSAAAERRRRRGA
LRRGGRRRAGAEGGAGGADGQGAGPGAAESGALTASRSPGPGGRLSRASSRSVEFFLSRR
RRARSSVCRRKVAQAREKRFTFVLAVVMGVFVLCWFPFFFSYSLYGICREACQVPGPLFK
FFFWIGYCNSSLNPVIYTVFNQDFRRSFKHILFRRRRRGFRQ
|
| Target 3 Number of Residues |
462 |
| Target 3 Molecular Weight |
49521.6 |
| Target 3 Theoretical pI |
10.69 |
| Target 3 GO Classification |
|
Function
|
amine receptor activity
adrenoceptor activity
alpha-adrenergic receptor activity
alpha2-adrenergic receptor activity
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity |
|
Process
|
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway |
|
Component
|
cell
membrane
intrinsic to membrane
integral to membrane |
|
| Target 3 General Function |
Involved in alpha2-adrenergic receptor activity |
| Target 3 Pathways |
Not Available |
| Target 3 Reactions |
Not Available |
| Target 3 Signals |
|
| Target 3 Transmembrane Regions |
- 52-76
- 89-114
- 125-147
- 169-191
- 208-231
- 380-407
- 421-441
|
| Target 3 Essentiality |
Non Essential |
| Target 3 Domain Function |
PF00001:7tm_1 |
| Target 3 GenBank ID Protein |
Not Available |
| Target 3 UniProtKB ID |
P18825 |
| Target 3 Cellular Location |
Cell membrane |
| Target 3 Gene Sequence |
>1386 bp
ATGGCGTCCCCGGCGCTGGCGGCGGCGCTGGCGGTGGCGGCAGCGGCGGGCCCCAATGCG
AGCGGCGCGGGCGAGAGGGGCAGCGGCGGGGTTGCCAATGCCTCGGGGGCTTCCTGGGGG
CCGCCGCGCGGCCAGTACTCGGCGGGCGCGGTGGCAGGGCTGGCTGCCGTGGTGGGCTTC
CTCATCGTCTTCACCGTGGTGGGCAACGTGCTGGTGGTGATCGCCGTGCTGACCAGCCGG
GCGCTGCGCGCGCCACAGAACCTCTTCCTGGTGTCGCTGGCCTCGGCCGACATCCTGGTG
GCCACGCTGGTCATGCCCTTCTCGTTGGCCAACGAGCTCATGGCCTACTGGTACTTCGGG
CAGGTGTGGTGCGGCGTGTACCTGGCGCTCGATGTGCTGTTTTGCACCTCGTCGATCGTG
CATCTGTGTGCCATCAGCCTGGACCGCTACTGGTCGGTGACGCAGGCCGTCGAGTACAAC
CTGAAGCGCACACCACGCCGCGTCAAGGCCACCATCGTCGCCGTGTGGCTCATCTCGGCC
GTCATCTCCTTCCCGCCGCTGGTCTCGCTCTACCGCCAGCCCGACGGCGCCGCCTACCCG
CAGTGCGGCCTCAACGACGAGACCTGGTACATCCTGTCCTCCTGCATCGGCTCCTTCTTC
GCGCCCTGCCTCATCATGGGCCTGGTCTACGCGCGCATCTACCGAGTGGCCAAGCGTCGC
ACGCGCACGCTCAGCGAGAAGCGCGCCCCCGTGGGCCCCGACGGTGCGTCCCCGACTACC
GAAAACGGGCTGGGCGCGGCGGCAGGCGAGGCGAGAACGGGCACTGCGCGCCCCCGCCCG
CCGACGTGGAGCCGGACGAGAGCAGCGCAGCGGCCGAGAGGCGGCGCGCCGGGGCCGTTG
CGGCGGGGCGGGCGGCGGCGAGCGGGCGCGGAGGGGGGCGCGGGCGGTGCGGACGGGCAG
GGGGCGGGGCCGGGGGCGGCTCAGTCGGGGGCGCTGACCGCCTCCAGGTCCCCGGGGCCC
GGTGGCCGCCTCTCGCGCGCCAGCTCGCGCTCCGTCGAGTTCTTCCTGTCGCGCCGGCGC
CGGGCGCGCAGCAGCGTGTGCCGCCGCAAGGTGGCCCAGGCGCGCGAGAAGCGCTTCACC
TTTGTGCTGGCTGTGGTCATGGGCGTGTTCGTGCTCTGCTGGTTCCCCTTCTTCTTCATC
TACAGCCTGTACGGCATCTGCCGCGAGGCCTGCCAGGTGCCCGGCCCGCTCTTCAAGTTC
TTCTTCTGGATCGGCTACTGCAACAGCTCGCTCAACCCGGTCATCTACACGGTCTTCAAC
CAGGATTTCCGGCCATCCTTCAAGCACATCCTCTTCCGACGGAGGAGAAGGGGCTTCAGG
CAGTGA
|
| Target 3 GenBank Gene ID |
Not Available |
| Target 3 GeneCard ID |
ADRA2C |
| Target 3 GenAtlas ID |
ADRA2C |
| Target 3 HGNC ID |
HGNC:283 |
| Target 3 Chromosome Location |
Not Available |
| Target 3 Locus |
4p16 |
| Target 3 SNPs |
SNPJam Report |
| Target 3 Toxin References |
- V520 - Zhang W, Ordway GA: The alpha2C-adrenoceptor modulates GABA release in mouse striatum. Brain Res Mol Brain Res. 2003 Apr 10;112(1-2):24-32. [PubMed ]
- V517 - Trendelenburg AU, Philipp M, Meyer A, Klebroff W, Hein L, Starke K: All three alpha2-adrenoceptor types serve as autoreceptors in postganglionic sympathetic neurons. Naunyn Schmiedebergs Arch Pharmacol. 2003 Dec;368(6):504-12. Epub 2003 Nov 11. [PubMed ]
- V519 - Orito K, Kishi M, Imaizumi T, Nakazawa T, Hashimoto A, Mori T, Kambe T: alpha(2)-adrenoceptor antagonist properties of OPC-28326, a novel selective peripheral vasodilator. Br J Pharmacol. 2001 Oct;134(4):763-70. [PubMed ]
- V521 - Prinster SC, Holmqvist TG, Hall RA: Alpha2C-adrenergic receptors exhibit enhanced surface expression and signaling upon association with beta2-adrenergic receptors. J Pharmacol Exp Ther. 2006 Sep;318(3):974-81. Epub 2006 Jun 6. [PubMed ]
|
| Target 3 General References |
2842764; 9371698; 10801795; 15319474; 1849485 |
