DT-Web

DB00940 - Methantheline


Identification
Name Methantheline
Accession Number DB00940 (APRD00751)
Type small molecule
Description Methantheline is a synthetic antispasmodic. Antispasmodics are used to relieve cramps or spasms of the stomach, intestines, and bladder. Methantheline is used to treat intestine or stomach ulcers (peptic ulcer disease), intestine problems (irritable bowel syndrome), pancreatitis, gastritis, biliary dyskinesia, pylorosplasm, or urinary problems (reflex neurogenic bladder in children).
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 340.436
Groups approved
Monoisotopic Weight 340.191268703
Pharmacology
Indication For the treatment of peptic ulcer disease, irritable bowel syndrome, pancreatitis, gastritis, biliary dyskinesia, pylorosplasm, and reflex neurogenic bladder in children.
Mechanism of action Methantheline inhibits the muscarinic actions of acetylcholine on structures innervated by postganglionic cholinergic nerves as well as on smooth muscles that respond to acetylcholine but lack cholinergic innervation. These postganglionic receptor sites are present in the autonomic effector cells of the smooth muscle, cardiac muscle, sinoatrial and atrioventricular nodes, and exocrine glands. Depending on the dose, anticholinergics may reduce the motility and secretory activity of the gastrointestinal system, and the tone of the ureter and urinary bladder and may have a slight relaxant action on the bile ducts and gallbladder.
Absorption Rapidly absorbed.
Protein binding Not Available
Biotransformation Hepatic, by enzymatic hydrolysis.
Route of elimination Not Available
Toxicity Symptoms of overdose: blurred vision (continuing) or changes in near vision, clumsiness or unsteadiness, confusion, convulsions, difficulty in breathing, muscle weakness (severe), or tiredness (severe), dizziness, drowsiness (severe), dryness of mouth, nose, or throat (severe), fast heartbeat, fever, hallucinations, slurred speech, unusual excitement, nervousness, restlessness, or irritability, unusual warmth, dryness, and flushing of skin.
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions
Drug Mechanism of interaction
Haloperidol The anticholinergic increases the risk of psychosis and tardive dyskinesia
Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Methantheline, may be reduced due to antagonism. The interaction may be beneficial when the anticholinergic action is a side effect. Monitor for decreased efficacy of both agents.
Trimethobenzamide Trimethobenzamide and Methantheline, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Triprolidine Triprolidine and Methantheline, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Trospium Trospium and Methantheline, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Food Interactions Not Available

Targets


Muscarinic acetylcholine receptor M1
Name Muscarinic acetylcholine receptor M1
Gene Name CHRM1
Pharmacological action unknown
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 0.4061
Histamine H2 receptor
Name Histamine H2 receptor
Gene Name HRH2
Pharmacological action yes
Actions antagonist
References
  • Hough LB, Barker LA: Histamine H2-receptor antagonism by propantheline and derivatives. J Pharmacol Exp Ther. 1981 Nov;219(2):453-8. - Pubmed
DTHybrid score 0.5632

Predictions


Id Partner name Gene Name Score
617 Muscarinic acetylcholine receptor M2 CHRM2 0.1304
51 Muscarinic acetylcholine receptor M3 CHRM3 0.1214
450 Muscarinic acetylcholine receptor M4 CHRM4 0.0708
274 Muscarinic acetylcholine receptor M5 CHRM5 0.0594
4119 Cytochrome P450 2D6 CYP2D6 0.0567
492 Histamine H1 receptor HRH1 0.052
1588 Multidrug resistance protein 1 ABCB1 0.0464
3923 Cholinesterase BCHE 0.041
4512 Cytochrome P450 3A4 CYP3A4 0.0398
6016 Cytochrome P450 2C19 CYP2C19 0.0339
502 5-hydroxytryptamine 2A receptor HTR2A 0.0328
6144 Solute carrier family 22 member 2 SLC22A2 0.0284
556 Alpha-1A adrenergic receptor ADRA1A 0.0283
831 D(2) dopamine receptor DRD2 0.0264
6142 Solute carrier family 22 member 8 SLC22A8 0.0253
4200 Cytochrome P450 1A2 CYP1A2 0.02
318 Alpha-2A adrenergic receptor ADRA2A 0.018
590 5-hydroxytryptamine 2C receptor HTR2C 0.0178
23 D(1A) dopamine receptor DRD1 0.0176
6145 Solute carrier family 22 member 1 SLC22A1 0.0175
716 5-hydroxytryptamine 7 receptor HTR7 0.0161
4757 Cytochrome P450 2C9 CYP2C9 0.0155
824 Sodium-dependent serotonin transporter SLC6A4 0.0147
540 Sodium-dependent noradrenaline transporter SLC6A2 0.0142
320 5-hydroxytryptamine 1A receptor HTR1A 0.0141
436 5-hydroxytryptamine 2B receptor HTR2B 0.0136
4118 Cytochrome P450 3A5 CYP3A5 0.0135
118 Organic cation/carnitine transporter 2 SLC22A5 0.0133
1341 Histamine H3 receptor HRH3 0.0121
6030 Cytochrome P450 2B6 CYP2B6 0.0117
164 Histamine H4 receptor HRH4 0.0117
1181 Alpha-1-acid glycoprotein 1 ORM1 0.011
6147 Solute carrier family 22 member 3 SLC22A3 0.0107
378 Alpha-2C adrenergic receptor ADRA2C 0.0105
629 Alpha-2B adrenergic receptor ADRA2B 0.0103
789 Alpha-1D adrenergic receptor ADRA1D 0.0102
6013 Cytochrome P450 2E1 CYP2E1 0.01
6104 Dimethylaniline monooxygenase [N-oxide-forming] 1 FMO1 0.0099
432 D(4) dopamine receptor DRD4 0.0096
833 Organic cation/carnitine transporter 1 SLC22A4 0.0094
813 Neuronal acetylcholine receptor subunit alpha-2 CHRNA2 0.0094
632 Alpha-1B adrenergic receptor ADRA1B 0.0094
4203 Histamine N-methyltransferase HNMT 0.0088
1656 CYP2B protein CYP2B 0.0087
638 D(3) dopamine receptor DRD3 0.0084
713 Sodium-dependent dopamine transporter SLC6A3 0.0082
1256 5-hydroxytryptamine 6 receptor HTR6 0.0078
4924 Cytochrome P450 2C8 CYP2C8 0.0078
805 Cytochrome P450 11B1, mitochondrial CYP11B1 0.0064
885 5-hydroxytryptamine 1B receptor HTR1B 0.0061
723 Cytosolic phospholipase A2 PLA2G4A 0.0057
6101 Dimethylaniline monooxygenase [N-oxide-forming] 3 FMO3 0.0051
6024 Cytochrome P450 1A1 CYP1A1 0.0051
6107 Cytochrome P450 3A7 CYP3A7 0.0049
706 Glutamate [NMDA] receptor subunit 3A GRIN3A 0.0049
6025 UDP-glucuronosyltransferase 1-4 UGT1A4 0.0047
6098 Potassium voltage-gated channel subfamily D member 2 KCND2 0.0046
6099 Potassium voltage-gated channel subfamily D member 3 KCND3 0.0046
5878 Alpha-7 nicotinic cholinergic receptor subunit CHRFAM7A 0.0044
2129 Sucrase-isomaltase, intestinal SI 0.0043
6154 Multidrug and toxin extrusion protein 1 SLC47A1 0.0041
458 Neuronal acetylcholine receptor subunit alpha-10 CHRNA10 0.004
528 5-hydroxytryptamine 1E receptor HTR1E 0.0038
193 Beta-1 adrenergic receptor ADRB1 0.0037
766 Beta-2 adrenergic receptor ADRB2 0.0036
94 5-hydroxytryptamine 4 receptor HTR4 0.0036
163 D(1B) dopamine receptor DRD5 0.0034
5718 Cytochrome P450 2A6 CYP2A6 0.0034
6023 Cytochrome P450 11B2, mitochondrial CYP11B2 0.0033
3876 Aromatic-L-amino-acid decarboxylase DDC 0.0033
380 Cytochrome P450 17A1 CYP17A1 0.0032
341 5-hydroxytryptamine 3 receptor HTR3A 0.003
220 Sodium channel protein type 5 subunit alpha SCN5A 0.003
776 Bile salt export pump ABCB11 0.0029
1024 Solute carrier family 22 member 11 SLC22A11 0.0029
725 5-hydroxytryptamine 1D receptor HTR1D 0.0028
6143 Solute carrier family 22 member 7 SLC22A7 0.0028
6176 UDP-glucuronosyltransferase 1-3 UGT1A3 0.0027
1729 Solute carrier family 22 member 6 SLC22A6 0.0023
465 Calmodulin CALM1 0.0022
215 Sodium channel protein type 11 subunit alpha SCN11A 0.0021
6432 Transporter snf 0.0018
3941 Amine oxidase [flavin-containing] A MAOA 0.0018
474 Acetylcholinesterase ACHE 0.0016
872 Gamma-aminobutyric-acid receptor subunit alpha-1 GABRA1 0.0015
587 Serum albumin ALB 0.0014
198 Sodium channel protein type 10 subunit alpha SCN10A 0.0014
6106 Cytochrome P450 2C18 CYP2C18 0.0013
1360 Sphingomyelin phosphodiesterase SMPD1 0.0012
6047 Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A PDE1A 0.0012
6100 BDNF/NT-3 growth factors receptor NTRK2 0.0011
5692 Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B PDE1B 0.0011
762 Voltage-dependent calcium channel subunit alpha-2/delta-1 CACNA2D1 0.0009
4110 Voltage-dependent L-type calcium channel subunit beta-2 CACNB2 0.0009
4115 Voltage-dependent L-type calcium channel subunit alpha-1D CACNA1D 0.0009
1618 High affinity nerve growth factor receptor NTRK1 0.0009
478 Voltage-dependent L-type calcium channel subunit alpha-1C CACNA1C 0.0008
1086 Potassium voltage-gated channel subfamily KQT member 2 KCNQ2 0.0008
734 D1 dopamine receptor-interacting protein calcyon CALY 0.0007
858 Potassium voltage-gated channel subfamily A member 1 KCNA1 0.0007
20 Prostaglandin G/H synthase 1 PTGS1 0.0006
467 Delta-type opioid receptor OPRD1 0.0005
696 Kappa-type opioid receptor OPRK1 0.0005
1898 Cytochrome P450 1B1 CYP1B1 0.0004
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