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Showing toxin card for Labetalol (T3D3517)

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Version 1.0
Creation Date 2009-07-30 17:58:59
Update Date 2010-05-18 21:03:54
Accession Number T3D3517
Name Labetalol
Compound Type
  • Adrenergic alpha-Antagonist
  • Adrenergic beta-Antagonist
  • Antihypertensive Agent
  • Drug
  • Sympatholytic
Description Blocker of both alpha- and beta-adrenergic receptors that is used as an antihypertensive. [PubChem]
Synonyms
  1. Labetalol HCL
  2. Labetalol hydrochloride
  3. Labetalolum [INN-Latin]
  4. Labetolol
Chemical IUPAC Name 2-hydroxy-5-{1-hydroxy-2-[(4-phenylbutan-2-yl)amino]ethyl}benzamide
Chemical Formula C19H24N2O3
Chemical Structure Structure
CAS Registry Number 36894-69-6
InChI Identifier InChI=1S/C19H24N2O3/c1-13(7-8-14-5-3-2-4-6-14)21-12-18(23)15-9-10-17(22)16(11-15)19(20)24/h2-6,9-11,13,18,21-23H,7-8,12H2,1H3,(H2,20,24)
InChI Key InChIKey=SGUAFYQXFOLMHL-UHFFFAOYSA-N
PubChem Compound ID 3869 Link Image
KEGG ID C07063 Link Image
UniProt ID Not Available
OMIM ID Not Available
ChEBI ID 6343 Link Image
BioCyc ID Not Available
SuperToxic ID Not Available
CTD ID Not Available
Stitch ID Labetalol Link Image
DrugBank ID DB00598 Link Image
PDB ID Not Available
ACToR ID Not Available
Wikipedia Link http://en.wikipedia.org/wiki/Labetalol Link Image
Monoisotopic Mass 328.178693
MOL File Show
PDB File Show
SDF File Show
SMILES CC(CCC1=CC=CC=C1)NCC(O)C1=CC=C(O)C(=C1)C(N)=O
Appearance Not Available
Melting Point 195-196 oC
Solubility 20 mg/ml (HCl salt)
Predicted LogP 1.3418
Route of Exposure Oral, parenteral (intravenous injection).
Mechanism of Action Labetalol has two asymmetric centers and therefore, exists as a molecular complex of two diastereoisomeric pairs. Dilevalol, the R,R' stereoisomer, makes up 25% of racemic labetalol. Labetalol HCl combines both selective, competitive, alpha-1-adrenergic blocking and nonselective, competitive, beta-adrenergic blocking activity in a single substance. In man, the ratios of alpha- to beta- blockade have been estimated to be approximately 1:3 and 1:7 following oral and intravenous (IV) administration, respectively. Beta-2-agonist activity has been demonstrated in animals with minimal beta-1-agonist (ISA) activity detected. In animals, at doses greater than those required for alpha- or beta- adrenergic blockade, a membrane stabilizing effect has been demonstrated.
Metabolism Primarily hepatic, undergoes significant first pass metabolism
Toxicity Values LD50 = 66 mg/kg (Rat, parental-intravenous)
Lethal Dose Not Available
Carcinogenicity (IARC Classification) Not Available
Uses/Sources Not Available
Minimum Risk Level Not Available
Health Effects Not Available
Symptoms Side effects or adverse reactions include dizziness when standing up, very low blood pressure, severely slow heartbeat, weakness, diminished sexual function, fatigue
Treatment Not Available
General References Not Available
Targets
  1. Alpha-1A adrenergic receptor
  2. Alpha-1B adrenergic receptor
  3. Beta-1 adrenergic receptor
  4. Beta-2 adrenergic receptor
Target 1 [top]
Target 1 ID 1142
Target 1 Name Alpha-1A adrenergic receptor
Target 1 Mechanism of Action Labetalol has two asymmetric centers and therefore, exists as a molecular complex of two diastereoisomeric pairs. Dilevalol, the R,R' stereoisomer, makes up 25% of racemic labetalol. Labetalol HCl combines both selective, competitive, alpha-1-adrenergic blocking and nonselective, competitive, beta-adrenergic blocking activity in a single substance. In man, the ratios of alpha- to beta- blockade have been estimated to be approximately 1:3 and 1:7 following oral and intravenous (IV) administration, respectively. Beta-2-agonist activity has been demonstrated in animals with minimal beta-1-agonist (ISA) activity detected. In animals, at doses greater than those required for alpha- or beta- adrenergic blockade, a membrane stabilizing effect has been demonstrated.
Target 1 Description This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol- calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins
Target 1 Synonyms
  1. Alpha 1A-adrenoreceptor; Alpha 1A-adrenoceptor; Alpha-1C adrenergic receptor; Alpha-adrenergic receptor 1c
Target 1 Gene Name ADRA1A
Target 1 Protein Sequence >Alpha-1A adrenergic receptor 
MVFLSGNASDSSNCTQPPAPVNISKAILLGVILGGLILFGVLGNILVILSVACHRHLHSV
THYYIVNLAVADLLLTSTVLPFSAIFEVLGYWAFGRVFCNIWAAVDVLCCTASIMGLCII
SIDRYIGVSYPLRYPTIVTQRRGLMALLCVWALSLVISIGPLFGWRQPAPEDETICQINE
EPGYVLFSALGSFYLPLAIILVMYCRVYVVAKRESRGLKSGLKTDKSDSEQVTLRIHRKN
APAGGSGMASAKTKTHFSVRLLKFSREKKAAKTLGIVVGCFVLCWLPFFLVMPIGSFFPD
FKPSETVFKIVFWLGYLNSCINPIIYPCSSQEFKKAFQNVLRIQCLCRKQSSKHALGYTL
HPPSQAVEGQHKDMVRIPVGSRETFYRISKTDGVCEWKFFSSMPRGSARITVSKDQSSCT
TARVRSKSFLQVCCCVGPSTPSLDKNHQVPTIKVHTISLSENGEEV
Target 1 Number of Residues 466
Target 1 Molecular Weight 51486.0
Target 1 Theoretical pI 9.23
Target 1 GO Classification
Function
amine receptor activity
adrenoceptor activity
alpha-adrenergic receptor activity
alpha1-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 alpha1-adrenergic receptor activity
Target 1 Pathways Not Available
Target 1 Reactions Not Available
Target 1 Signals
  • None
Target 1 Transmembrane Regions
  • 28-51
  • 65-88
  • 100-122
  • 144-167
  • 182-205
  • 274-297
  • 306-329
Target 1 Essentiality Non Essential
Target 1 Domain Function PF00001:7tm_1
Target 1 GenBank ID Protein Not Available
Target 1 UniProtKB ID P35348 Link Image
Target 1 Cellular Location Cell membrane
Target 1 Gene Sequence >1401 bp 
ATGGTGTTTCTCTCGGGAAATGCTTCCGACAGCTCCAACTGCACCCAACCGCCGGCACCG
GTGAACATTTCCAAGGCCATTCTGCTCGGGGTGATCTTGGGGGGCCTCATTCTTTTCGGG
GTGCTGGGTAACATCCTAGTGATCCTCTCCGTAGCCTGTCACCGACACCTGCACTCAGTC
ACGCACTACTACATCGTCAACCTGGCGGTGGCCGACCTCCTGCTCACCTCCACGGTGCTG
CCCTTCTCCGCCATCTTCGAGGTCCTAGGCTACTGGGCCTTCGGCAGGGTCTTCTGCAAC
ATCTGGGCGGCAGTGGATGTGCTGTGCTGCACCGCGTCCATCATGGGCCTCTGCATCATC
TCCATCGACCGCTACATCGGCGTGAGCTACCCGCTGCGCTACCCAACCATCGTCACCCAG
AGGAGGGGTCTCATGGCTCTGCTCTGCGTCTGGGCACTCTCCCTGGTCATATCCATTGGA
CCCCTGTTCGGCTGGAGGCAGCCGGCCCCCGAGGACGAGACCATCTGCCAGATCAACGAG
GAGCCGGGCTACGTGCTCTTCTCAGCGCTGGGCTCCTTCTACCTGCCTCTGGCCATCATC
CTGGTCATGTACTGCCGCGTCTACGTGGTGGCCAAGAGGGAGAGCCGGGGCCTCAAGTCT
GGCCTCAAGACCGACAAGTCGGACTCGGAGCAAGTGACGCTCCGCATCCATCGGAAAAAC
GCCCCGGCAGGAGGCAGCGGGATGGCCAGCGCCAAGACCAAGACGCACTTCTCAGTGAGG
CTCCTCAAGTTCTCCCGGGAGAAGAAAGCGGCCAAAACGCTGGGCATCGTGGTCGGCTGC
TTCGTCCTCTGCTGGCTGCCTTTTTTCTTAGTCATGCCCATTGGGTCTTTCTTCCCTGAT
TTCAAGCCCTCTGAAACAGTTTTTAAAATAGTATTTTGGCTCGGATATCTAAACAGCTGC
ATCAACCCCATCATATACCCATGCTCCAGCCAAGAGTTCAAAAAGGCCTTTCAGAATGTC
TTGAGAATCCAGTGTCTCCGCAGAAAGCAGTCTTCCAAACATGCCCTGGGCTACACCCTG
CACCCGCCCAGCCAGGCCGTGGAAGGGCAACACAAGGACATGGTGCGCATCCCCGTGGGA
TCAAGAGAGACCTTCTACAGGATCTCCAAGACGGATGGCGTTTGTGAATGGAAATTTTTC
TCTTCCATGCCCCGTGGATCTGCCAGGATTACAGTGTCCAAAGACCAATCCTCCTGTACC
ACAGCCCGGGTGAGAAGTAAAAGCTTTTTGGAGGTCTGCTGCTGTGTAGGGCCCTCAACC
CCCAGCCTTGACAAGAACCATCAAGTTCCAACCATTAAGGTCCACACCATCTCCCTCAGT
GAGAACGGGGAGGAAGTCTAG
Target 1 GenBank Gene ID Not Available
Target 1 GeneCard ID ADRA1A Link Image
Target 1 GenAtlas ID ADRA1A Link Image
Target 1 HGNC ID HGNC:277 Link Image
Target 1 Chromosome Location Not Available
Target 1 Locus 8p21-p11.2
Target 1 SNPs SNPJam Report Link Image
Target 1 Toxin References Not Available
Target 1 General References 8396931; 8024574; 8183249; 8564208; 7815325; 7737411; 9490024; 10493934
Target 2 [top]
Target 2 ID 1193
Target 2 Name Alpha-1B adrenergic receptor
Target 2 Mechanism of Action Labetalol has two asymmetric centers and therefore, exists as a molecular complex of two diastereoisomeric pairs. Dilevalol, the R,R' stereoisomer, makes up 25% of racemic labetalol. Labetalol HCl combines both selective, competitive, alpha-1-adrenergic blocking and nonselective, competitive, beta-adrenergic blocking activity in a single substance. In man, the ratios of alpha- to beta- blockade have been estimated to be approximately 1:3 and 1:7 following oral and intravenous (IV) administration, respectively. Beta-2-agonist activity has been demonstrated in animals with minimal beta-1-agonist (ISA) activity detected. In animals, at doses greater than those required for alpha- or beta- adrenergic blockade, a membrane stabilizing effect has been demonstrated.
Target 2 Description This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol- calcium second messenger system
Target 2 Synonyms
  1. Alpha 1B-adrenoreceptor; Alpha 1B-adrenoceptor
Target 2 Gene Name ADRA1B
Target 2 Protein Sequence >Alpha-1B adrenergic receptor 
MNPDLDTGHNTSAPAHWGELKNANFTGPNQTSSNSTLPQLDITRAISVGLVLGAFILFAI
VGNILVILSVACNRHLRTPTNYFIVNLAMADLLLSFTVLPFSAALEVLGYWVLGRIFCDI
WAAVDVLCCTASILSLCAISIDRYIGVRYSLQYPTLVTRRKAILALLSVWVLSTVISIGP
LLGWKEPAPNDDKECGVTEEPFYALFSSLGSFYIPLAVILVMYCRVYIVAKRTTKNLEAG
VMKEMSNSKELTLRIHSKNFHEDTLSSTKAKGHNPRSSIAVKLFKFSREKKAAKTLGIVV
GMFILCWLPFFIALPLGSLFSTLKPPDAVFKVVFWLGYFNSCLNPIIYPCSSKEFKRAFV
RILGCQCRGRGRRRRRRRRRLGGCAYTYRPWTRGGSLERSQSRKDSLDDSGSCLSGSQRT
LPSASPSPGYLGRGAPPPVELCAFPEWKAPGALLSLPAPEPPGRRGRHDSGPLFTFKLLT
EPESPGTDGGASNGGCEAAADVANGQPGFKSNMPLAPGQF
Target 2 Number of Residues 520
Target 2 Molecular Weight 56835.4
Target 2 Theoretical pI 9.79
Target 2 GO Classification
Function
amine receptor activity
adrenoceptor activity
alpha-adrenergic receptor activity
alpha1-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 alpha1-adrenergic receptor activity
Target 2 Pathways Not Available
Target 2 Reactions Not Available
Target 2 Signals
  • None
Target 2 Transmembrane Regions
  • 46-70
  • 84-105
  • 116-141
  • 162-184
  • 202-224
  • 296-319
  • 327-351
Target 2 Essentiality Non Essential
Target 2 Domain Function PF00001:7tm_1
Target 2 GenBank ID Protein Not Available
Target 2 UniProtKB ID P35368 Link Image
Target 2 Cellular Location Cell membrane
Target 2 Gene Sequence >1563 bp 
ATGAATCCCGACCTGGACACCGGCCACAACACATCAGCACCTGCCCACTGGGGAGAGTTG
AAAAATGCCAACTTCACTGGCCCCAACCAGACCTCGAGCAACTCCACACTGCCCCAGCTG
GACATCACCAGGGCCATCTCTGTGGGCCTGGTGCTGGGCGCCTTCATCCTCTTTGCCATC
GTGGGCAACATCCTAGTCATCTTGTCTGTGGCCTGCAACCGGCACCTGCGGACGCCCACC
AACTACTTCATTGTCAACCTGGCCATGGCCGACCTGCTGTTGAGCTTCACCGTCCTGCCC
TTCTCAGCGGCCCTAGAGGTGCTCGGCTACTGGGTGCTGGGGCGGATCTTCTGTGACATC
TGGGCAGCCGTGGATGTCCTGTGCTGCACAGCGTCCATTCTGAGCCTGTGCGCCATCTCC
ATCGATCGCTACATCGGGGTGCGCTACTCTCTGCAGTATCCCACGCTGGTCACCCGGAGG
AAGGCCATCTTGGCGCTGCTCAGTGTCTGGGTCTTGTCCACCGTCATCTCCATCGGGCCT
CTCCTTGGGTGGAAGGAGCCGGCACCCAACGATGACAAGGAGTGCGGGGTCACCGAAGAA
CCCTTCTATGCCCTCTTCTCCTCTCTGGGCTCCTTCTACATCCCTCTGGCGGTCATTCTA
GTCATGTACTGCCGTGTCTATATAGTGGCCAAGAGAACCACCAAGAACCTAGAGGCAGGA
GTCATGAAGGAGATGTCCAACTCCAAGGAGCTGACCCTGAGGATCCATTCCAAGAACTTT
CACGAGGACACCCTTAGCAGTACCAAGGCCAAGGGCCACAACCCCAGGAGTTCCATAGCT
GTCAAACTTTTTAAGTTCTCCAGGGAAAAGAAAGCAGCTAAGACGTTGGGCATTGTGGTC
GGTATGTTCATCTTGTGCTGGCTACCCTTCTTCATCGCTCTACCGCTTGGCTCCTTGTTC
TCCACCCTGAAGCCCCCCGACGCCGTGTTCAAGGTGGTGTTCTGGCTGGGCTACTTCAAC
AGCTGCCTCAACCCCATCATCTACCCATGCTCCAGCAAGGAGTTCAAGCGCGCTTTCGTG
CGCATCCTCGGGTGCCAGTGCCGCGGCCGCGGCCGCCGCCGACGCCGCCGCCGCCGTCGC
CTGGGCGGCTGCGCCTACACCTACCGGCCGTGGACGCGCGGCGGCTCGCTGGAGCGCTCG
CAGTCGCGCAAGGACTCGCTGGACGACAGCGGCAGCTGCCTGAGCGGCAGCCAGCGGACC
CTGCCCTCGGCCTCGCCGAGCCCGGGCTACCTGGGCCGCGGCGCGCCACCGCCAGTCGAG
CTGTGCGCCTTCCCCGAGTGGAAGGCGCCCGGCGCCCTCCTGAGCCTGCCCGCGCCTGAG
CCCCCCGGCCGCCGCGGCCGCCACGACTCGGGCCCGCTCTTCACCTTCAAGCTCCTGACC
GAGCCCGAGAGCCCCGGGACCGACGGCGGCGCCAGCAACGGAGGCTGCGAGGCCGCGGCC
GACGTGGCCAACGGGCAGCCGGGCTTCAAAAGCAACATGCCCCTGGCGCCCGGGCAGTTT
TAG
Target 2 GenBank Gene ID Not Available
Target 2 GeneCard ID ADRA1B Link Image
Target 2 GenAtlas ID ADRA1B Link Image
Target 2 HGNC ID HGNC:278 Link Image
Target 2 Chromosome Location Not Available
Target 2 Locus 5q23-q32
Target 2 SNPs SNPJam Report Link Image
Target 2 Toxin References Not Available
Target 2 General References 1328250; 8183249; 7815325
Target 3 [top]
Target 3 ID 1175
Target 3 Name Beta-1 adrenergic receptor
Target 3 Mechanism of Action Labetalol has two asymmetric centers and therefore, exists as a molecular complex of two diastereoisomeric pairs. Dilevalol, the R,R' stereoisomer, makes up 25% of racemic labetalol. Labetalol HCl combines both selective, competitive, alpha-1-adrenergic blocking and nonselective, competitive, beta-adrenergic blocking activity in a single substance. In man, the ratios of alpha- to beta- blockade have been estimated to be approximately 1:3 and 1:7 following oral and intravenous (IV) administration, respectively. Beta-2-agonist activity has been demonstrated in animals with minimal beta-1-agonist (ISA) activity detected. In animals, at doses greater than those required for alpha- or beta- adrenergic blockade, a membrane stabilizing effect has been demonstrated.
Target 3 Description Beta-adrenergic receptors mediate the catecholamine- induced activation of adenylate cyclase through the action of G proteins. This receptor binds epinephrine and norepinephrine with approximately equal affinity
Target 3 Synonyms
  1. Beta-1 adrenoreceptor; Beta-1 adrenoceptor
Target 3 Gene Name ADRB1
Target 3 Protein Sequence >Beta-1 adrenergic receptor 
MGAGVLVLGASEPGNLSSAAPLPDGAATAARLLVPASPPASLLPPASESPEPLSQQWTAG
MGLLMALIVLLIVAGNVLVIVAIAKTPRLQTLTNLFIMSLASADLVMGLLVVPFGATIVV
WGRWEYGSFFCELWTSVDVLCVTASIETLCVIALDRYLAITSPFRYQSLLTRARARGLVC
TVWAISALVSFLPILMHWWRAESDEARRCYNDPKCCDFVTNRAYAIASSVVSFYVPLCIM
AFVYLRVFREAQKQVKKIDSCERRFLGGPARPPSPSPSPVPAPAPPPGPPRPAAAAATAP
LANGRAGKRRPSRLVALREQKALKTLGIIMGVFTLCWLPFFLANVVKAFHRELVPDRLFV
FFNWLGYANSAFNPIIYCRSPDFRKAFQRLLCCARRAARRRHATHGDRPRASGCLARPGP
PPSPGAASDDDDDDVVGATPPARLLEPWAGCNGGAAADSDSSLDEPCRPGFASESKV
Target 3 Number of Residues 477
Target 3 Molecular Weight 51322.1
Target 3 Theoretical pI 9.03
Target 3 GO Classification
Function
amine receptor activity
adrenoceptor activity
beta-adrenergic receptor activity
beta1-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 beta1-adrenergic receptor activity
Target 3 Pathways Not Available
Target 3 Reactions Not Available
Target 3 Signals
  • None
Target 3 Transmembrane Regions
  • 56-84
  • 94-120
  • 133-154
  • 173-196
  • 223-248
  • 320-349
  • 355-377
Target 3 Essentiality Non Essential
Target 3 Domain Function PF00001:7tm_1
Target 3 GenBank ID Protein Not Available
Target 3 UniProtKB ID P08588 Link Image
Target 3 Cellular Location Cell membrane
Target 3 Gene Sequence >1434 bp 
CCCCGGCCTCCGCAGCTCGGCATGGGCGCGGGGGTGCTCGTCCTGGGCGCCTCCGAGCCC
GGTAACCTGTCGTCGGCCGCACCGCTCCCCGACGGCGCGGCCACCGCGGCGCGGCTGCTG
GTGCCCGCGTCGCCGCCCGCCTCGTTGCTGCCTCCCGCCAGCGAAAGCCCCGAGCCGCTG
TCTCAGCAGTGGACAGCGGGCATGGGTCTGCTGATGGCGCTCATCGTGCTGCTCATCGTG
GCGGGCAATGTGCTGGTGATCGTGGCCATCGCCAAGACGCCGCGGCTGCAGACGCTCACC
AACCTCTTCATCATGTCCCTGGCCAGCGCCGACCTGGTCATGGGGCTGCTGGTGGTGCCG
TTCGGGGCCACCATCGTGGTGTGGGGCCGCTGGGAGTACGGCTCCTTCTTCTGCGAGCTG
TGGACCTCAGTGGACGTGCTGTGCGTGACGGCCAGCATCGAGACCCTGTGTGTCATTGCC
CTGGACCGCTACCTCGCCATCACCTCGCCCTTCCGCTACCAGAGCCTGCTGACGCGCGCG
CGGGCGCGGGGCCTCGTGTGCACCGTGTGGGCCATCTCGGCCCTGGTGTCCTTCCTGCCC
ATCCTCATGCACTGGTGGCGGGCGGAGAGCGACGAGGCGCGCCGCTGCTACAACGACCCC
AAGTGCTGCGACTTCGTCACCAACCGGGCCTACGCCATCGCCTCGTCCGTAGTCTCCTTC
TACGTGCCCCTGTGCATCATGGCCTTCGTGTACCTGCGGGTGTTCCGCGAGGCCCAGAAG
CAGGTGAAGAAGATCGACAGCTGCGAGCGCCGTTTCCTCGGCGGCCCAGCGCGGCCGCCC
TCGCCCTCGCCCTCGCCCGTCCCCGCGCCCGCGCCGCCGCCCGGACCCCCGCGCCCCGCC
GCCGCCGCCGCCACCGCCCCGCTGGCCAACGGGCGTGCGGGTAAGCGGCGGCCCTCGCGC
CTCGTGGCCCTACGCGAGCAGAAGGCGCTCAAGACGCTGGGCATCATCATGGGCGTCTTC
ACGCTCTGCTGGCTGCCCTTCTTCCTGGCCAACGTGGTGAAGGCCTTCCACCGCGAGCTG
GTGCCCGACCGCCTCTTCGTCTTCTTCAACTGGCTGGGCTACGCCAACTCGGCCTTCAAC
CCCATCATCTACTGCCGCAGCCCCGACTTCCGCAAGGCCTTCCAGGGACTGCTCTGCTGC
GCGCGCAGGGCTGCCCGCCGGCGCCACGCGACCCACGGAGACCGGCCGCGCGCCTCGGGC
TGTCTGGCCCGGCCCGGACCCCCGCCATCGCCCGGGGCCGCCTCGGACGACGACGACGAC
GATGTCGTCGGGGCCACGCCGCCCGCGCGCCTGCTGGAGCCCTGGGCCGGCTGCAACGGC
GGGGCGGCGGCGGACAGCGACTCGAGCCTGGACGAGCCGTGCCGCCCCGGCTTC
Target 3 GenBank Gene ID Not Available
Target 3 GeneCard ID ADRB1 Link Image
Target 3 GenAtlas ID ADRB1 Link Image
Target 3 HGNC ID HGNC:285 Link Image
Target 3 Chromosome Location Chromosome:10
Target 3 Locus 10q24-q26
Target 3 SNPs SNPJam Report Link Image
Target 3 Toxin References Not Available
Target 3 General References 2825170; 10477438; 15164054; 15358775; 10212248; 11052857; 11854867
Target 4 [top]
Target 4 ID 1303
Target 4 Name Beta-2 adrenergic receptor
Target 4 Mechanism of Action Labetalol has two asymmetric centers and therefore, exists as a molecular complex of two diastereoisomeric pairs. Dilevalol, the R,R' stereoisomer, makes up 25% of racemic labetalol. Labetalol HCl combines both selective, competitive, alpha-1-adrenergic blocking and nonselective, competitive, beta-adrenergic blocking activity in a single substance. In man, the ratios of alpha- to beta- blockade have been estimated to be approximately 1:3 and 1:7 following oral and intravenous (IV) administration, respectively. Beta-2-agonist activity has been demonstrated in animals with minimal beta-1-agonist (ISA) activity detected. In animals, at doses greater than those required for alpha- or beta- adrenergic blockade, a membrane stabilizing effect has been demonstrated.
Target 4 Description Beta-adrenergic receptors mediate the catecholamine- induced activation of adenylate cyclase through the action of G proteins. The beta-2-adrenergic receptor binds epinephrine with an approximately 30-fold greater affinity than it does norepinephrine
Target 4 Synonyms
  1. Beta-2 adrenoreceptor; Beta-2 adrenoceptor
Target 4 Gene Name ADRB2
Target 4 Protein Sequence >Beta-2 adrenergic receptor 
MGQPGNGSAFLLAPNGSHAPDHDVTQQRDEVWVVGMGIVMSLIVLAIVFGNVLVITAIAK
FERLQTVTNYFITSLACADLVMGLAVVPFGAAHILMKMWTFGNFWCEFWTSIDVLCVTAS
IETLCVIAVDRYFAITSPFKYQSLLTKNKARVIILMVWIVSGLTSFLPIQMHWYRATHQE
AINCYANETCCDFFTNQAYAIASSIVSFYVPLVIMVFVYSRVFQEAKRQLQKIDKSEGRF
HVQNLSQVEQDGRTGHGLRRSSKFCLKEHKALKTLGIIMGTFTLCWLPFFIVNIVHVIQD
NLIRKEVYILLNWIGYVNSGFNPLIYCRSPDFRIAFQELLCLRRSSLKAYGNGYSSNGNT
GEQSGYHVEQEKENKLLCEDLPGTEDFVGHQGTVPSDNIDSPGRNCSTNDSLL
Target 4 Number of Residues 413
Target 4 Molecular Weight 46426.3
Target 4 Theoretical pI 7.23
Target 4 GO Classification
Function
amine receptor activity
adrenoceptor activity
beta-adrenergic receptor activity
beta2-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 4 General Function Involved in beta2-adrenergic receptor activity
Target 4 Pathways Not Available
Target 4 Reactions Not Available
Target 4 Signals
  • None
Target 4 Transmembrane Regions
  • 35-58
  • 72-95
  • 107-129
  • 151-174
  • 197-220
  • 275-298
  • 306-329
Target 4 Essentiality Non Essential
Target 4 Domain Function PF00001:7tm_1
Target 4 GenBank ID Protein Not Available
Target 4 UniProtKB ID P07550 Link Image
Target 4 Cellular Location Cell membrane
Target 4 Gene Sequence >1242 bp 
ATGGGGCAACCCGGGAACGGCAGCGCCTTCTTGCTGGCACCCAATGGAAGCCATGCGCCG
GACCACGACGTCACGCAGGAAAGGGACGAGGTGTGGGTGGTGGGCATGGGCATCGTCATG
TCTCTCATCGTCCTGGCCATCGTGTTTGGCAATGTGCTGGTCATCACAGCCATTGCCAAG
TTCGAGCGTCTGCAGACGGTCACCAACTACTTCATCACTTCACTGGCCTGTGCTGATCTG
GTCATGGGCCTGGCAGTGGTGCCCTTTGGGGCCGCCCATATTCTTATGAAAATGTGGACT
TTTGGCAACTTCTGGTGCGAGTTTTGGACTTCCATTGATGTGCTGTGCGTCACGGCCAGC
ATTGAGACCCTGTGCGTGATCGCAGTGGATCGCTACTTTGCCATTACTTCACCTTTCAAG
TACCAGAGCCTGCTGACCAAGAATAAGGCCCGGGTGATCATTCTGATGGTGTGGATTGTG
TCAGGCCTTACCTCCTTCTTGCCCATTCAGATGCACTGGTACCGGGCCACCCACCAGGAA
GCCATCAACTGCTATGCCAATGAGACCTGCTGTGACTTCTTCACGAACCAAGCCTATGCC
ATTGCCTCTTCCATCGTGTCCTTCTACGTTCCCCTGGTGATCATGGTCTTCGTCTACTCC
AGGGTCTTTCAGGAGGCCAAAAGGCAGCTCCAGAAGATTGACAAATCTGAGGGCCGCTTC
CATGTCCAGAACCTTAGCCAGGTGGAGCAGGATGGGCGGACGGGGCATGGACTCCGCAGA
TCTTCCAAGTTCTGCTTGAAGGAGCACAAAGCCCTCAAGACGTTAGGCATCATCATGGGC
ACTTTCACCCTCTGCTGGCTGCCCTTCTTCATCGTTAACATTGTGCATGTGATCCAGGAT
AACCTCATCCGTAAGGAAGTTTACATCCTCCTAAATTGGATAGGCTATGTCAATTCTGGT
TTCAATCCCCTTATCTACTGCCGGAGCCCAGATTTCAGGATTGCCTTCCAGGAGCTTCTG
TGCCTGCGCAGGTCTTCTTTGAAGGCCTATGGGAATGGCTACTCCAGCAACGGCAACACA
GGGGAGCAGAGTGGATATCACGTGGAACAGGAGAAAGAAAATAAACTGCTGTGTGAAGAC
CTCCCAGGCACGGAAGACTTTGTGGGCCATCAAGGTACTGTGCCTAGCGATAACATTGAT
TCACAAGGGAGGAATTGTAGTACAAATGACTCACTGCTGTAA
Target 4 GenBank Gene ID Not Available
Target 4 GeneCard ID ADRB2 Link Image
Target 4 GenAtlas ID ADRB2 Link Image
Target 4 HGNC ID HGNC:286 Link Image
Target 4 Chromosome Location Not Available
Target 4 Locus 5q31-q32
Target 4 SNPs SNPJam Report Link Image
Target 4 Toxin References Not Available
Target 4 General References 3026848; 3034889; 3033609; 3025863; 2823249; 8383511; 11246467; 14702039

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