DT-Web

DB00217 - Bethanidine


Identification
Name Bethanidine
Accession Number DB00217 (APRD00825)
Type small molecule
Description A guanidinium antihypertensive agent that acts by blocking adrenergic transmission.
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 177.2462
Groups approved
Monoisotopic Weight 177.126597495
Pharmacology
Indication For the treatment of hypertension.
Mechanism of action Bethanidine, a guanidine derivative, is a peripherally acting antiadrenergic agent which primarily acts as an alpha2a adrenergic agonist. Bethanidine effectively decreases blood pressure by suppressing renin secretion or interfering with function of the sympathetic nervous system.
Absorption Absorbed rapidly in the gastrointestinal tract following oral administration.
Protein binding Not Available
Biotransformation Not Available
Route of elimination Not Available
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions Not Available
Food Interactions Not Available

Targets


Alpha-2C adrenergic receptor
Name Alpha-2C adrenergic receptor
Gene Name ADRA2C
Pharmacological action yes
Actions agonist
References
  • Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. - Pubmed
  • 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. - Pubmed
  • Noshiro T, Miura Y, Kimura S, Meguro Y, Sugawara T, Ohashi H, Takahashi M, Sano N, Watanabe H, Ohzeki T, et al.: Functional relationships between platelet alpha 2-adrenoceptors and sympathetic nerve activity in clinical hypertensive states. J Hypertens. 1990 Dec;8(12):1097-104. - Pubmed
  • Noshiro T, Miura Y, Kimura S, Meguro Y, Sugawara T, Ohashi H, Takahashi M, Sano N, Watanabe H, Ohzeki T, et al.: Functional relationship between platelet alpha 2-adrenoceptors and sympathetic nerve activity in man. Clin Exp Hypertens A. 1989;11 Suppl 1:287-94. - Pubmed
DTHybrid score 0.3105
Alpha-2A adrenergic receptor
Name Alpha-2A adrenergic receptor
Gene Name ADRA2A
Pharmacological action unknown
Actions agonist
References
  • Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. - Pubmed
  • 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. - Pubmed
DTHybrid score 0.4282
Alpha-2B adrenergic receptor
Name Alpha-2B adrenergic receptor
Gene Name ADRA2B
Pharmacological action unknown
Actions agonist
References
  • Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. - Pubmed
  • 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. - Pubmed
DTHybrid score 0.2987
ATP-sensitive inward rectifier potassium channel 1
Name ATP-sensitive inward rectifier potassium channel 1
Gene Name KCNJ1
Pharmacological action yes
Actions inhibitor
References
  • Bkaily G, Caille JP, Payet MD, Peyrow M, Sauve R, Renaud JF, Sperelakis N: Bethanidine increases one type of potassium current and relaxes aortic muscle. Can J Physiol Pharmacol. 1988 Jun;66(6):731-6. - Pubmed
  • Bkaily G: Bethanidine, nitroprusside and atrial natriuretic factor open a cGMP-sensitive K+ channel in aortic muscle. Prog Clin Biol Res. 1990;327:507-15. - Pubmed
DTHybrid score 0.5856

Predictions


Id Partner name Gene Name Score
556 Alpha-1A adrenergic receptor ADRA1A 0.1549
230 ATP-binding cassette transporter sub-family C member 8 ABCC8 0.1106
23 D(1A) dopamine receptor DRD1 0.106
502 5-hydroxytryptamine 2A receptor HTR2A 0.0987
320 5-hydroxytryptamine 1A receptor HTR1A 0.0937
831 D(2) dopamine receptor DRD2 0.0904
163 D(1B) dopamine receptor DRD5 0.0878
590 5-hydroxytryptamine 2C receptor HTR2C 0.0864
632 Alpha-1B adrenergic receptor ADRA1B 0.086
638 D(3) dopamine receptor DRD3 0.0853
725 5-hydroxytryptamine 1D receptor HTR1D 0.0812
432 D(4) dopamine receptor DRD4 0.0801
4512 Cytochrome P450 3A4 CYP3A4 0.0778
885 5-hydroxytryptamine 1B receptor HTR1B 0.0733
4119 Cytochrome P450 2D6 CYP2D6 0.0685
5251 Carbonyl reductase [NADPH] 1 CBR1 0.0661
4200 Cytochrome P450 1A2 CYP1A2 0.064
789 Alpha-1D adrenergic receptor ADRA1D 0.0629
6070 Nischarin NISCH 0.0605
436 5-hydroxytryptamine 2B receptor HTR2B 0.0538
716 5-hydroxytryptamine 7 receptor HTR7 0.048
492 Histamine H1 receptor HRH1 0.0461
6147 Solute carrier family 22 member 3 SLC22A3 0.0445
540 Sodium-dependent noradrenaline transporter SLC6A2 0.0424
766 Beta-2 adrenergic receptor ADRB2 0.0419
6145 Solute carrier family 22 member 1 SLC22A1 0.0393
781 ATP-sensitive inward rectifier potassium channel 11 KCNJ11 0.039
20 Prostaglandin G/H synthase 1 PTGS1 0.0387
4757 Cytochrome P450 2C9 CYP2C9 0.0382
193 Beta-1 adrenergic receptor ADRB1 0.0363
6144 Solute carrier family 22 member 2 SLC22A2 0.0348
1588 Multidrug resistance protein 1 ABCB1 0.0324
824 Sodium-dependent serotonin transporter SLC6A4 0.0314
1517 Beta-3 adrenergic receptor ADRB3 0.0265
713 Sodium-dependent dopamine transporter SLC6A3 0.0263
1256 5-hydroxytryptamine 6 receptor HTR6 0.0263
6020 Aldehyde oxidase AOX1 0.0258
131 Synaptic vesicular amine transporter SLC18A2 0.0256
3941 Amine oxidase [flavin-containing] A MAOA 0.0232
3970 Voltage-dependent N-type calcium channel subunit alpha-1B CACNA1B 0.0231
274 Muscarinic acetylcholine receptor M5 CHRM5 0.0223
4118 Cytochrome P450 3A5 CYP3A5 0.0223
6016 Cytochrome P450 2C19 CYP2C19 0.0218
401 Glutamate [NMDA] receptor subunit zeta-1 GRIN1 0.0218
450 Muscarinic acetylcholine receptor M4 CHRM4 0.0217
828 Phenylalanine-4-hydroxylase PAH 0.0211
3109 Phenylalanine-4-hydroxylase phhA 0.0211
118 Organic cation/carnitine transporter 2 SLC22A5 0.0203
103 Muscarinic acetylcholine receptor M1 CHRM1 0.0201
51 Muscarinic acetylcholine receptor M3 CHRM3 0.0195
528 5-hydroxytryptamine 1E receptor HTR1E 0.0194
617 Muscarinic acetylcholine receptor M2 CHRM2 0.019
1539 Oligopeptide transporter, small intestine isoform SLC15A1 0.0178
341 5-hydroxytryptamine 3 receptor HTR3A 0.0175
3939 Amine oxidase [flavin-containing] B MAOB 0.0171
1632 Solute carrier organic anion transporter family member 2B1 SLCO2B1 0.017
6107 Cytochrome P450 3A7 CYP3A7 0.014
734 D1 dopamine receptor-interacting protein calcyon CALY 0.0134
1974 Oligopeptide transporter, kidney isoform SLC15A2 0.012
124 Histamine H2 receptor HRH2 0.0112
6139 Solute carrier organic anion transporter family member 1A2 SLCO1A2 0.0111
1636 Trace amine-associated receptor 1 TAAR1 0.011
6024 Cytochrome P450 1A1 CYP1A1 0.0108
6013 Cytochrome P450 2E1 CYP2E1 0.0101
1181 Alpha-1-acid glycoprotein 1 ORM1 0.0099
1729 Solute carrier family 22 member 6 SLC22A6 0.0098
6164 POU domain, class 5, transcription factor 1 POU5F1 0.0097
465 Calmodulin CALM1 0.0097
3961 G protein-activated inward rectifier potassium channel 4 KCNJ5 0.0095
4924 Cytochrome P450 2C8 CYP2C8 0.0095
872 Gamma-aminobutyric-acid receptor subunit alpha-1 GABRA1 0.0094
3876 Aromatic-L-amino-acid decarboxylase DDC 0.0091
6106 Cytochrome P450 2C18 CYP2C18 0.009
1680 Solute carrier family 2, facilitated glucose transporter member 1 SLC2A1 0.0089
587 Serum albumin ALB 0.0087
3810 Catechol O-methyltransferase COMT 0.0083
6025 UDP-glucuronosyltransferase 1-4 UGT1A4 0.0077
521 ATP-binding cassette transporter sub-family C member 9 ABCC9 0.0074
6023 Cytochrome P450 11B2, mitochondrial CYP11B2 0.0073
233 Potassium channel subfamily K member 2 KCNK2 0.0072
833 Organic cation/carnitine transporter 1 SLC22A4 0.0069
132 ATP-binding cassette sub-family A member 1 ABCA1 0.0067
6151 Monocarboxylate transporter 10 SLC16A10 0.0066
805 Cytochrome P450 11B1, mitochondrial CYP11B1 0.0064
6101 Dimethylaniline monooxygenase [N-oxide-forming] 3 FMO3 0.0063
2184 Cystic fibrosis transmembrane conductance regulator CFTR 0.0063
4114 Voltage-dependent L-type calcium channel subunit beta-3 CACNB3 0.0061
4112 Voltage-dependent L-type calcium channel subunit beta-4 CACNB4 0.0061
6030 Cytochrome P450 2B6 CYP2B6 0.0061
4113 Voltage-dependent L-type calcium channel subunit alpha-1F CACNA1F 0.0057
333 Voltage-dependent L-type calcium channel subunit beta-1 CACNB1 0.0056
158 Sodium channel protein type 1 subunit alpha SCN1A 0.0054
3811 Cytochrome P450 19A1 CYP19A1 0.0052
4110 Voltage-dependent L-type calcium channel subunit beta-2 CACNB2 0.0048
4115 Voltage-dependent L-type calcium channel subunit alpha-1D CACNA1D 0.0048
4111 Voltage-dependent L-type calcium channel subunit alpha-1S CACNA1S 0.0047
3426 Glutamine synthetase glnA 0.0047
3987 Glutamine synthetase GLUL 0.0047
478 Voltage-dependent L-type calcium channel subunit alpha-1C CACNA1C 0.0046
3923 Cholinesterase BCHE 0.0046
101 Potassium voltage-gated channel subfamily H member 2 KCNH2 0.0044
1709 Canalicular multispecific organic anion transporter 2 ABCC3 0.0042
776 Bile salt export pump ABCB11 0.004
6143 Solute carrier family 22 member 7 SLC22A7 0.0039
164 Histamine H4 receptor HRH4 0.0039
4120 NADPH--cytochrome P450 reductase POR 0.0037
862 Multidrug resistance-associated protein 1 ABCC1 0.0037
1735 Canalicular multispecific organic anion transporter 1 ABCC2 0.0034
1732 ATP-binding cassette sub-family G member 2 ABCG2 0.0034
696 Kappa-type opioid receptor OPRK1 0.0026
1898 Cytochrome P450 1B1 CYP1B1 0.0023
1656 CYP2B protein CYP2B 0.0021
5718 Cytochrome P450 2A6 CYP2A6 0.0019
6100 BDNF/NT-3 growth factors receptor NTRK2 0.0013
1618 High affinity nerve growth factor receptor NTRK1 0.001
1086 Potassium voltage-gated channel subfamily KQT member 2 KCNQ2 0.001
6098 Potassium voltage-gated channel subfamily D member 2 KCND2 0.001
6099 Potassium voltage-gated channel subfamily D member 3 KCND3 0.001
858 Potassium voltage-gated channel subfamily A member 1 KCNA1 0.0008
467 Delta-type opioid receptor OPRD1 0.0007
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