DT-Web

DB01616 - Alverine


Identification
Name Alverine
Accession Number DB01616
Type small molecule
Description Alverine is a smooth muscle relaxant. Smooth muscle is a type of muscle that is not under voluntary control; it is the muscle present in places such as the gut and uterus. Alverine acts directly on the muscle in the gut, causing it to relax. This prevents the muscle spasms which occur in the gut in conditions such as irritable bowel syndrome and diverticular disease. It is used to relieve cramps or spasms of the stomach and intestines. It is also useful in treating irritable bowel syndrome (IBS) and similar conditions. It can also be used to help relieve period pain. Alverine is formulated as the citrate salt (5982-87-6).
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 281.4351
Groups approved
Monoisotopic Weight 281.214349869
Pharmacology
Indication Used to relieve cramps or spasms of the stomach and intestines. It is also useful in treating irritable bowel syndrome (IBS) and similar conditions. It can also be used to help relieve period pain. Alverine citrate is also under investigation to increase the cytotoxic effects of the proteasome inhibitor MG132 on breast cancer cells.
Mechanism of action Not Available
Absorption Not Available
Protein binding Not Available
Biotransformation Rapidly converted to its primary active metabolite, which is then further converted to two secondary metabolites.
Route of elimination High renal clearance of all metabolites indicating that they are eliminated by active renal secretion.
Toxicity Can produce hypotension and atropine-like toxic effects. Fatality has occurred following overdose with very high doses.
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions
Drug Mechanism of interaction
Donepezil Possible antagonism of action
Galantamine Possible antagonism of action
Food Interactions Not Available

Targets


5-hydroxytryptamine 1A receptor
Name 5-hydroxytryptamine 1A receptor
Gene Name HTR1A
Pharmacological action yes
Actions antagonist
References
  • Coelho AM, Jacob L, Fioramonti J, Bueno L: Rectal antinociceptive properties of alverine citrate are linked to antagonism at the 5-HT1A receptor subtype. J Pharm Pharmacol. 2001 Oct;53(10):1419-26. - Pubmed
DTHybrid score 0.181

Predictions


Id Partner name Gene Name Score
502 5-hydroxytryptamine 2A receptor HTR2A 0.0582
885 5-hydroxytryptamine 1B receptor HTR1B 0.0501
831 D(2) dopamine receptor DRD2 0.0459
725 5-hydroxytryptamine 1D receptor HTR1D 0.0373
4119 Cytochrome P450 2D6 CYP2D6 0.0368
23 D(1A) dopamine receptor DRD1 0.0334
4512 Cytochrome P450 3A4 CYP3A4 0.0329
318 Alpha-2A adrenergic receptor ADRA2A 0.0323
590 5-hydroxytryptamine 2C receptor HTR2C 0.031
556 Alpha-1A adrenergic receptor ADRA1A 0.0288
378 Alpha-2C adrenergic receptor ADRA2C 0.0283
629 Alpha-2B adrenergic receptor ADRA2B 0.0268
638 D(3) dopamine receptor DRD3 0.0264
193 Beta-1 adrenergic receptor ADRB1 0.0257
766 Beta-2 adrenergic receptor ADRB2 0.0251
432 D(4) dopamine receptor DRD4 0.025
716 5-hydroxytryptamine 7 receptor HTR7 0.0248
436 5-hydroxytryptamine 2B receptor HTR2B 0.0226
511 5-hydroxytryptamine 1F receptor HTR1F 0.0216
632 Alpha-1B adrenergic receptor ADRA1B 0.0212
163 D(1B) dopamine receptor DRD5 0.0192
4200 Cytochrome P450 1A2 CYP1A2 0.0174
94 5-hydroxytryptamine 4 receptor HTR4 0.0159
1588 Multidrug resistance protein 1 ABCB1 0.0153
492 Histamine H1 receptor HRH1 0.015
4118 Cytochrome P450 3A5 CYP3A5 0.0145
1181 Alpha-1-acid glycoprotein 1 ORM1 0.0134
824 Sodium-dependent serotonin transporter SLC6A4 0.0128
6107 Cytochrome P450 3A7 CYP3A7 0.0127
3941 Amine oxidase [flavin-containing] A MAOA 0.0125
103 Muscarinic acetylcholine receptor M1 CHRM1 0.0114
6145 Solute carrier family 22 member 1 SLC22A1 0.0104
587 Serum albumin ALB 0.0102
1517 Beta-3 adrenergic receptor ADRB3 0.0094
1256 5-hydroxytryptamine 6 receptor HTR6 0.009
6016 Cytochrome P450 2C19 CYP2C19 0.0089
528 5-hydroxytryptamine 1E receptor HTR1E 0.0084
274 Muscarinic acetylcholine receptor M5 CHRM5 0.0072
450 Muscarinic acetylcholine receptor M4 CHRM4 0.007
341 5-hydroxytryptamine 3 receptor HTR3A 0.0069
789 Alpha-1D adrenergic receptor ADRA1D 0.0068
4757 Cytochrome P450 2C9 CYP2C9 0.0065
51 Muscarinic acetylcholine receptor M3 CHRM3 0.0062
617 Muscarinic acetylcholine receptor M2 CHRM2 0.0061
6013 Cytochrome P450 2E1 CYP2E1 0.0061
540 Sodium-dependent noradrenaline transporter SLC6A2 0.0059
6106 Cytochrome P450 2C18 CYP2C18 0.0054
1632 Solute carrier organic anion transporter family member 2B1 SLCO2B1 0.0052
734 D1 dopamine receptor-interacting protein calcyon CALY 0.0039
713 Sodium-dependent dopamine transporter SLC6A3 0.0034
6144 Solute carrier family 22 member 2 SLC22A2 0.0029
1490 Solute carrier organic anion transporter family member 1B1 SLCO1B1 0.0025
1656 CYP2B protein CYP2B 0.0025
124 Histamine H2 receptor HRH2 0.0025
6139 Solute carrier organic anion transporter family member 1A2 SLCO1A2 0.0025
20 Prostaglandin G/H synthase 1 PTGS1 0.0025
1732 ATP-binding cassette sub-family G member 2 ABCG2 0.0024
6025 UDP-glucuronosyltransferase 1-4 UGT1A4 0.0023
5718 Cytochrome P450 2A6 CYP2A6 0.0021
847 Mu-type opioid receptor OPRM1 0.0021
6024 Cytochrome P450 1A1 CYP1A1 0.0019
6101 Dimethylaniline monooxygenase [N-oxide-forming] 3 FMO3 0.0018
6100 BDNF/NT-3 growth factors receptor NTRK2 0.0016
776 Bile salt export pump ABCB11 0.0016
3923 Cholinesterase BCHE 0.0014
1618 High affinity nerve growth factor receptor NTRK1 0.0013
6098 Potassium voltage-gated channel subfamily D member 2 KCND2 0.0012
6099 Potassium voltage-gated channel subfamily D member 3 KCND3 0.0012
1086 Potassium voltage-gated channel subfamily KQT member 2 KCNQ2 0.0012
164 Histamine H4 receptor HRH4 0.0011
4924 Cytochrome P450 2C8 CYP2C8 0.001
858 Potassium voltage-gated channel subfamily A member 1 KCNA1 0.001
467 Delta-type opioid receptor OPRD1 0.0008
696 Kappa-type opioid receptor OPRK1 0.0008
1898 Cytochrome P450 1B1 CYP1B1 0.0007
6030 Cytochrome P450 2B6 CYP2B6 0.0006
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