DT-Web

DB01625 - Isopropamide


Identification
Name Isopropamide
Accession Number DB01625
Type small molecule
Description Isopropamide iodide is a long-acting quaternary anticholinergic drug. It is used in the treatment of peptic ulcer and other gastrointestinal disorders marked by hyperacidity and hypermotility.
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 353.5209
Groups approved
Monoisotopic Weight 353.259288688
Pharmacology
Indication For the treatment of a wide range of gastrointestinal disorders, including such conditions as peptic ulcer, gastritis, hyperchlorhydria, functional diarrhea, irritable or spastic colon, pyloroduodenal irritability, pylorospasm, acute nonspecific gastroenteritis, biliary dyskinesia and chronic cholelithiasis, duodenitis, gastrointestinal spasm; it may also be used to treat genitourinary spasm.
Mechanism of action Anticholinergics are a class of medications that inhibit parasympathetic nerve impulses by selectively blocking the binding of the neurotransmitter acetylcholine to its receptor in nerve cells. The nerve fibers of the parasympathetic system are responsible for the involuntary movements of smooth muscles present in the gastrointestinal tract. Inhibition here decreases acidity and motility, aiding in the treatment of gastrointestinal disorders.
Absorption Not Available
Protein binding Not Available
Biotransformation Not Available
Route of elimination Not Available
Toxicity Symptoms of overdose include dryness of mouth, dysphagia, thirst, blurred vision, dilated pupils, photophobia, fever, rapid pulse and respiration, disorientation. Depression and circulatory collapse may result from severe overdosage.
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions
Drug Mechanism of interaction
Donepezil Possible antagonism of action
Galantamine Possible antagonism of action
Haloperidol The anticholinergic increases the risk of psychosis and tardive dyskinesia
Food Interactions Not Available

Targets


Muscarinic acetylcholine receptor M3
Name Muscarinic acetylcholine receptor M3
Gene Name CHRM3
Pharmacological action yes
Actions antagonist
References
  • Eglen RM, Whiting RL: Competitive and non-competitive antagonism exhibited by 'selective' antagonists at atrial and ileal muscarinic receptor subtypes. Br J Pharmacol. 1987 Apr;90(4):701-7. - Pubmed
  • Lane MA: Muscarinic cholinergic activation of mouse spleen cells cytotoxic to tumor cells in vitro. J Natl Cancer Inst. 1978 Sep;61(3):923-6. - Pubmed
DTHybrid score 0.399
Muscarinic acetylcholine receptor M4
Name Muscarinic acetylcholine receptor M4
Gene Name CHRM4
Pharmacological action unknown
Actions antagonist
References
  • Lane MA: Muscarinic cholinergic activation of mouse spleen cells cytotoxic to tumor cells in vitro. J Natl Cancer Inst. 1978 Sep;61(3):923-6. - Pubmed
  • Eglen RM, Whiting RL: Competitive and non-competitive antagonism exhibited by 'selective' antagonists at atrial and ileal muscarinic receptor subtypes. Br J Pharmacol. 1987 Apr;90(4):701-7. - Pubmed
DTHybrid score 0.2753

Predictions


Id Partner name Gene Name Score
617 Muscarinic acetylcholine receptor M2 CHRM2 0.2603
103 Muscarinic acetylcholine receptor M1 CHRM1 0.2493
274 Muscarinic acetylcholine receptor M5 CHRM5 0.1763
492 Histamine H1 receptor HRH1 0.0508
4119 Cytochrome P450 2D6 CYP2D6 0.0505
4512 Cytochrome P450 3A4 CYP3A4 0.0466
502 5-hydroxytryptamine 2A receptor HTR2A 0.0382
556 Alpha-1A adrenergic receptor ADRA1A 0.0329
1588 Multidrug resistance protein 1 ABCB1 0.031
590 5-hydroxytryptamine 2C receptor HTR2C 0.0289
831 D(2) dopamine receptor DRD2 0.0244
3923 Cholinesterase BCHE 0.0242
4200 Cytochrome P450 1A2 CYP1A2 0.0231
789 Alpha-1D adrenergic receptor ADRA1D 0.0229
4757 Cytochrome P450 2C9 CYP2C9 0.0228
632 Alpha-1B adrenergic receptor ADRA1B 0.0213
6016 Cytochrome P450 2C19 CYP2C19 0.021
23 D(1A) dopamine receptor DRD1 0.0208
540 Sodium-dependent noradrenaline transporter SLC6A2 0.0197
432 D(4) dopamine receptor DRD4 0.0192
1181 Alpha-1-acid glycoprotein 1 ORM1 0.0177
6030 Cytochrome P450 2B6 CYP2B6 0.0169
6013 Cytochrome P450 2E1 CYP2E1 0.0169
813 Neuronal acetylcholine receptor subunit alpha-2 CHRNA2 0.0159
638 D(3) dopamine receptor DRD3 0.0157
824 Sodium-dependent serotonin transporter SLC6A4 0.0155
320 5-hydroxytryptamine 1A receptor HTR1A 0.0137
2129 Sucrase-isomaltase, intestinal SI 0.0135
4924 Cytochrome P450 2C8 CYP2C8 0.0134
378 Alpha-2C adrenergic receptor ADRA2C 0.0133
318 Alpha-2A adrenergic receptor ADRA2A 0.0132
629 Alpha-2B adrenergic receptor ADRA2B 0.0131
4118 Cytochrome P450 3A5 CYP3A5 0.0123
528 5-hydroxytryptamine 1E receptor HTR1E 0.012
1256 5-hydroxytryptamine 6 receptor HTR6 0.0111
163 D(1B) dopamine receptor DRD5 0.0108
833 Organic cation/carnitine transporter 1 SLC22A4 0.0104
716 5-hydroxytryptamine 7 receptor HTR7 0.0101
341 5-hydroxytryptamine 3 receptor HTR3A 0.0095
6098 Potassium voltage-gated channel subfamily D member 2 KCND2 0.0092
6099 Potassium voltage-gated channel subfamily D member 3 KCND3 0.0092
725 5-hydroxytryptamine 1D receptor HTR1D 0.0089
885 5-hydroxytryptamine 1B receptor HTR1B 0.0088
6144 Solute carrier family 22 member 2 SLC22A2 0.0086
5878 Alpha-7 nicotinic cholinergic receptor subunit CHRFAM7A 0.0084
6145 Solute carrier family 22 member 1 SLC22A1 0.0083
118 Organic cation/carnitine transporter 2 SLC22A5 0.0073
6107 Cytochrome P450 3A7 CYP3A7 0.0072
436 5-hydroxytryptamine 2B receptor HTR2B 0.007
465 Calmodulin CALM1 0.0068
6104 Dimethylaniline monooxygenase [N-oxide-forming] 1 FMO1 0.0067
5718 Cytochrome P450 2A6 CYP2A6 0.0059
6432 Transporter snf 0.0057
458 Neuronal acetylcholine receptor subunit alpha-10 CHRNA10 0.005
587 Serum albumin ALB 0.0044
6106 Cytochrome P450 2C18 CYP2C18 0.004
1360 Sphingomyelin phosphodiesterase SMPD1 0.004
6147 Solute carrier family 22 member 3 SLC22A3 0.0039
6101 Dimethylaniline monooxygenase [N-oxide-forming] 3 FMO3 0.0039
6047 Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A PDE1A 0.0036
467 Delta-type opioid receptor OPRD1 0.0036
696 Kappa-type opioid receptor OPRK1 0.0036
6100 BDNF/NT-3 growth factors receptor NTRK2 0.0035
6176 UDP-glucuronosyltransferase 1-3 UGT1A3 0.0034
5692 Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B PDE1B 0.0034
762 Voltage-dependent calcium channel subunit alpha-2/delta-1 CACNA2D1 0.0028
6182 Cytochrome P450 2J2 CYP2J2 0.0028
4110 Voltage-dependent L-type calcium channel subunit beta-2 CACNB2 0.0027
1618 High affinity nerve growth factor receptor NTRK1 0.0027
4115 Voltage-dependent L-type calcium channel subunit alpha-1D CACNA1D 0.0027
478 Voltage-dependent L-type calcium channel subunit alpha-1C CACNA1C 0.0026
1086 Potassium voltage-gated channel subfamily KQT member 2 KCNQ2 0.0026
124 Histamine H2 receptor HRH2 0.0024
164 Histamine H4 receptor HRH4 0.0024
734 D1 dopamine receptor-interacting protein calcyon CALY 0.0023
220 Sodium channel protein type 5 subunit alpha SCN5A 0.0023
101 Potassium voltage-gated channel subfamily H member 2 KCNH2 0.0022
858 Potassium voltage-gated channel subfamily A member 1 KCNA1 0.0021
706 Glutamate [NMDA] receptor subunit 3A GRIN3A 0.0021
20 Prostaglandin G/H synthase 1 PTGS1 0.002
193 Beta-1 adrenergic receptor ADRB1 0.0018
847 Mu-type opioid receptor OPRM1 0.0018
766 Beta-2 adrenergic receptor ADRB2 0.0018
6025 UDP-glucuronosyltransferase 1-4 UGT1A4 0.0018
1898 Cytochrome P450 1B1 CYP1B1 0.0014
6024 Cytochrome P450 1A1 CYP1A1 0.0011
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