DT-Web

DB00785 - Cryptenamine


Identification
Name Cryptenamine
Accession Number DB00785 (APRD00890)
Type small molecule
Description Cryptenamine is a mixture of closely related hypotensive alkaloids from Veratrum album (Liliaceae). It has been used in the treatment of hypertension but has largely been replaced by drugs with fewer adverse effects. Cryptenamine has a marked and re-producible depressor effect when given intravenously to hypertensive patients, however the mechanism of action is not known.
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight Not Available
Groups approved
Monoisotopic Weight Not Available
Pharmacology
Indication For the treatment of hypertension.
Mechanism of action Cryptenamine has a marked and re-producible depressor effect when given intravenously to hypertensive patients, however the mechanism of action is not known. Some evidence has suggested that cryptenamine acts in a similar fashion to atropine, which lowers the "rest and digest" activity of all muscles and glands regulated by the parasympathetic nervous system. This occurs because atropine is a competitive inhibitor of the muscarinic acetylcholine receptors (acetylcholine is the neurotransmitter used by the parasympathetic nervous system). Therefore muscarinic acetylcholine receptors will be listed as experimental targets for cryptenamine.
Absorption Not Available
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


Muscarinic acetylcholine receptor M2
Name Muscarinic acetylcholine receptor M2
Gene Name CHRM2
Pharmacological action yes
Actions antagonist
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
  • Jandhyala ML, Buckley JP: Mechanisms of action of cryptenamine. J Pharm Sci. 1968 Sep;57(9):1576-82. - Pubmed
  • Jandhyala BS, Buckley JP: Pharmacology and mechanism of action of cryptenamine. J Pharm Sci. 1966 Sep;55(9):888-93. - Pubmed
DTHybrid score 0.7545
Muscarinic acetylcholine receptor M1
Name Muscarinic acetylcholine receptor M1
Gene Name CHRM1
Pharmacological action yes
Actions antagonist
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 0.8625
Muscarinic acetylcholine receptor M3
Name Muscarinic acetylcholine receptor M3
Gene Name CHRM3
Pharmacological action yes
Actions antagonist
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 0.7578
Muscarinic acetylcholine receptor M4
Name Muscarinic acetylcholine receptor M4
Gene Name CHRM4
Pharmacological action yes
Actions antagonist
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 0.5385
Muscarinic acetylcholine receptor M5
Name Muscarinic acetylcholine receptor M5
Gene Name CHRM5
Pharmacological action yes
Actions antagonist
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 0.4382

Predictions


Id Partner name Gene Name Score
492 Histamine H1 receptor HRH1 0.1453
4119 Cytochrome P450 2D6 CYP2D6 0.1343
4512 Cytochrome P450 3A4 CYP3A4 0.1117
502 5-hydroxytryptamine 2A receptor HTR2A 0.0985
556 Alpha-1A adrenergic receptor ADRA1A 0.0839
1588 Multidrug resistance protein 1 ABCB1 0.0799
3923 Cholinesterase BCHE 0.0794
813 Neuronal acetylcholine receptor subunit alpha-2 CHRNA2 0.0764
831 D(2) dopamine receptor DRD2 0.0735
590 5-hydroxytryptamine 2C receptor HTR2C 0.0685
23 D(1A) dopamine receptor DRD1 0.0597
4200 Cytochrome P450 1A2 CYP1A2 0.0552
6016 Cytochrome P450 2C19 CYP2C19 0.0541
789 Alpha-1D adrenergic receptor ADRA1D 0.0539
4757 Cytochrome P450 2C9 CYP2C9 0.0536
540 Sodium-dependent noradrenaline transporter SLC6A2 0.051
632 Alpha-1B adrenergic receptor ADRA1B 0.0501
432 D(4) dopamine receptor DRD4 0.0452
1181 Alpha-1-acid glycoprotein 1 ORM1 0.0441
824 Sodium-dependent serotonin transporter SLC6A4 0.043
6013 Cytochrome P450 2E1 CYP2E1 0.0418
6030 Cytochrome P450 2B6 CYP2B6 0.0389
638 D(3) dopamine receptor DRD3 0.037
320 5-hydroxytryptamine 1A receptor HTR1A 0.0364
318 Alpha-2A adrenergic receptor ADRA2A 0.0327
4924 Cytochrome P450 2C8 CYP2C8 0.0323
2129 Sucrase-isomaltase, intestinal SI 0.0317
378 Alpha-2C adrenergic receptor ADRA2C 0.0312
629 Alpha-2B adrenergic receptor ADRA2B 0.0309
4118 Cytochrome P450 3A5 CYP3A5 0.0296
528 5-hydroxytryptamine 1E receptor HTR1E 0.0281
341 5-hydroxytryptamine 3 receptor HTR3A 0.027
833 Organic cation/carnitine transporter 1 SLC22A4 0.0267
1256 5-hydroxytryptamine 6 receptor HTR6 0.0261
163 D(1B) dopamine receptor DRD5 0.0255
436 5-hydroxytryptamine 2B receptor HTR2B 0.0245
716 5-hydroxytryptamine 7 receptor HTR7 0.0237
6098 Potassium voltage-gated channel subfamily D member 2 KCND2 0.0229
6099 Potassium voltage-gated channel subfamily D member 3 KCND3 0.0229
6145 Solute carrier family 22 member 1 SLC22A1 0.0223
6144 Solute carrier family 22 member 2 SLC22A2 0.0218
725 5-hydroxytryptamine 1D receptor HTR1D 0.021
885 5-hydroxytryptamine 1B receptor HTR1B 0.0206
118 Organic cation/carnitine transporter 2 SLC22A5 0.0193
5878 Alpha-7 nicotinic cholinergic receptor subunit CHRFAM7A 0.018
6107 Cytochrome P450 3A7 CYP3A7 0.0167
124 Histamine H2 receptor HRH2 0.0163
465 Calmodulin CALM1 0.0159
5718 Cytochrome P450 2A6 CYP2A6 0.0151
458 Neuronal acetylcholine receptor subunit alpha-10 CHRNA10 0.0136
6432 Transporter snf 0.0133
6024 Cytochrome P450 1A1 CYP1A1 0.013
706 Glutamate [NMDA] receptor subunit 3A GRIN3A 0.0127
723 Cytosolic phospholipase A2 PLA2G4A 0.0124
6104 Dimethylaniline monooxygenase [N-oxide-forming] 1 FMO1 0.012
587 Serum albumin ALB 0.0102
713 Sodium-dependent dopamine transporter SLC6A3 0.0096
6106 Cytochrome P450 2C18 CYP2C18 0.0095
1360 Sphingomyelin phosphodiesterase SMPD1 0.0093
6176 UDP-glucuronosyltransferase 1-3 UGT1A3 0.0093
6147 Solute carrier family 22 member 3 SLC22A3 0.0092
6101 Dimethylaniline monooxygenase [N-oxide-forming] 3 FMO3 0.0091
220 Sodium channel protein type 5 subunit alpha SCN5A 0.0088
1656 CYP2B protein CYP2B 0.0087
6047 Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A PDE1A 0.0086
6100 BDNF/NT-3 growth factors receptor NTRK2 0.0082
5692 Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B PDE1B 0.0081
474 Acetylcholinesterase ACHE 0.0079
762 Voltage-dependent calcium channel subunit alpha-2/delta-1 CACNA2D1 0.0065
4110 Voltage-dependent L-type calcium channel subunit beta-2 CACNB2 0.0064
1618 High affinity nerve growth factor receptor NTRK1 0.0064
4115 Voltage-dependent L-type calcium channel subunit alpha-1D CACNA1D 0.0064
478 Voltage-dependent L-type calcium channel subunit alpha-1C CACNA1C 0.0062
1086 Potassium voltage-gated channel subfamily KQT member 2 KCNQ2 0.0061
467 Delta-type opioid receptor OPRD1 0.0059
696 Kappa-type opioid receptor OPRK1 0.0058
164 Histamine H4 receptor HRH4 0.0057
734 D1 dopamine receptor-interacting protein calcyon CALY 0.0054
858 Potassium voltage-gated channel subfamily A member 1 KCNA1 0.0049
20 Prostaglandin G/H synthase 1 PTGS1 0.0047
215 Sodium channel protein type 11 subunit alpha SCN11A 0.0045
193 Beta-1 adrenergic receptor ADRB1 0.0043
766 Beta-2 adrenergic receptor ADRB2 0.0042
6025 UDP-glucuronosyltransferase 1-4 UGT1A4 0.0042
94 5-hydroxytryptamine 4 receptor HTR4 0.0036
6139 Solute carrier organic anion transporter family member 1A2 SLCO1A2 0.0036
6023 Cytochrome P450 11B2, mitochondrial CYP11B2 0.0033
3876 Aromatic-L-amino-acid decarboxylase DDC 0.0033
1898 Cytochrome P450 1B1 CYP1B1 0.0033
380 Cytochrome P450 17A1 CYP17A1 0.0032
198 Sodium channel protein type 10 subunit alpha SCN10A 0.003
805 Cytochrome P450 11B1, mitochondrial CYP11B1 0.0029
6182 Cytochrome P450 2J2 CYP2J2 0.0028
101 Potassium voltage-gated channel subfamily H member 2 KCNH2 0.0022
847 Mu-type opioid receptor OPRM1 0.0018
3941 Amine oxidase [flavin-containing] A MAOA 0.0018
872 Gamma-aminobutyric-acid receptor subunit alpha-1 GABRA1 0.0015
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