DT-Web

DB00411 - Carbachol


Identification
Name Carbachol
Accession Number DB00411 (APRD00845, DB02487)
Type small molecule
Description A slowly hydrolyzed cholinergic agonist that acts at both muscarinic and nicotinic receptors. [PubChem]
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 182.649
Groups approved
Monoisotopic Weight 182.082205441
Pharmacology
Indication Primarily used in the treatment of glaucoma, but is also used during ophthalmic surgery.
Mechanism of action Carbachol is a parasympathomimetic that stimulates both muscarinic and nicotinic receptors. In topical ocular and intraocular administration its principal effects are miosis and increased aqueous humour outflow.
Absorption Not well absorbed in the gastro-intestinal tract, and does not cross the blood-brain barrier.
Protein binding Not Available
Biotransformation Not Available
Route of elimination Not Available
Toxicity Oral, mouse: LD50 = 15 mg/kg; Oral, rat: LD50 = 40 mg/kg.
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions
Drug Mechanism of interaction
Tacrine The acetylcholinesterase inhibitor, Tacrine, may increase the cholinergic effects of Carbachol, a cholinergic agonist. Monitor for increased cholinergic effects.
Food Interactions Not Available

Targets


Muscarinic acetylcholine receptor M1
Name Muscarinic acetylcholine receptor M1
Gene Name CHRM1
Pharmacological action yes
Actions agonist
References
  • Weiner DM, Goodman MW, Colpitts TM, Feddock MA, Duggento KL, Nash NR, Levey AI, Brann MR: Functional screening of drug target genes: m1 muscarinic acetylcholine receptor phenotypes in degenerative dementias. Am J Pharmacogenomics. 2004;4(2):119-28. - Pubmed
DTHybrid score 0.555
Muscarinic acetylcholine receptor M2
Name Muscarinic acetylcholine receptor M2
Gene Name CHRM2
Pharmacological action yes
Actions agonist
References
  • Peter JC, Wallukat G, Tugler J, Maurice D, Roegel JC, Briand JP, Hoebeke J: Modulation of the M2 muscarinic acetylcholine receptor activity with monoclonal anti-M2 receptor antibody fragments. J Biol Chem. 2004 Dec 31;279(53):55697-706. Epub 2004 Oct 14. - Pubmed
  • May LT, Lin Y, Sexton PM, Christopoulos A: Regulation of M2 muscarinic acetylcholine receptor expression and signaling by prolonged exposure to allosteric modulators. J Pharmacol Exp Ther. 2005 Jan;312(1):382-90. Epub 2004 Aug 27. - Pubmed
  • Sawatzky DA, Kingham PJ, Durcan N, McLean WG, Costello RW: Eosinophil-induced release of acetylcholine from differentiated cholinergic nerve cells. Am J Physiol Lung Cell Mol Physiol. 2003 Dec;285(6):L1296-304. Epub 2003 Aug 29. - Pubmed
  • Sterin-Borda L, Joensen L, Bayo-Hanza C, Esteva M, Borda E: Therapeutic use of muscarinic acetylcholine receptor peptide to prevent mice chagasic cardiac dysfunction. J Mol Cell Cardiol. 2002 Dec;34(12):1645-54. - Pubmed
  • Zuchner T, Schliebs R, Perez-Polo JR: Down-regulation of muscarinic acetylcholine receptor M2 adversely affects the expression of Alzheimer's disease-relevant genes and proteins. J Neurochem. 2005 Oct;95(1):20-32. - Pubmed
DTHybrid score 0.5143
Neuronal acetylcholine receptor subunit alpha-2
Name Neuronal acetylcholine receptor subunit alpha-2
Gene Name CHRNA2
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
  • An MC, Lin W, Yang J, Dominguez B, Padgett D, Sugiura Y, Aryal P, Gould TW, Oppenheim RW, Hester ME, Kaspar BK, Ko CP, Lee KF: Acetylcholine negatively regulates development of the neuromuscular junction through distinct cellular mechanisms. Proc Natl Acad Sci U S A. 2010 Jun 8;107(23):10702-7. Epub 2010 May 24. - Pubmed
  • Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. - Pubmed
DTHybrid score 0.6325

Enzymes


Cytosolic phospholipase A2
Name Cytosolic phospholipase A2
Gene Name PLA2G4A
Actions inducer
References
  • Konrad RJ, Jolly YC, Major C, Wolf BA: Carbachol stimulation of phospholipase A2 and insulin secretion in pancreatic islets. Biochem J. 1992 Oct 1;287 ( Pt 1):283-90. - Pubmed
  • Enyedi P, Fredholm BB: Calcium-dependent enhancement by carbachol of the VIP-induced cyclic AMP accumulation in cat submandibular gland. Acta Physiol Scand. 1984 Apr;120(4):523-8. - Pubmed
  • Grosfils K, Gomez F, Dehaye JP: Inhibition by mepacrine and amylase secretion from intact and permeabilized rat pancreatic acini. Biochem Biophys Res Commun. 1992 Apr 15;184(1):408-13. - Pubmed
  • Ying Z, Tojo H, Nonaka Y, Okamoto M: Cloning and expression of phospholipase A2 from guinea pig gastric mucosa, its induction by carbachol and secretion in vivo. Eur J Biochem. 1993 Jul 1;215(1):91-7. - Pubmed
  • Strosznajder J, Strosznajder RP: Guanine nucleotides and fluoride enhance carbachol-mediated arachidonic acid release from phosphatidylinositol. Evidence for involvement of GTP-binding protein in phospholipase A2 activation. J Lipid Mediat. 1989 Jul-Aug;1(4):217-29. - Pubmed
  • Hirasawa N, Santini F, Beaven MA: Activation of the mitogen-activated protein kinase/cytosolic phospholipase A2 pathway in a rat mast cell line. Indications of different pathways for release of arachidonic acid and secretory granules. J Immunol. 1995 May 15;154(10):5391-402. - Pubmed
  • Strosznajder J, Samochocki M: Carbachol-stimulated release of arachidonic acid and eicosanoids from brain cortex synaptoneurosome lipids of adult and aged rats. Adv Exp Med Biol. 1992;318:251-8. - Pubmed
DTHybrid score 0.4015

Predictions


Id Partner name Gene Name Score
51 Muscarinic acetylcholine receptor M3 CHRM3 0.2858
450 Muscarinic acetylcholine receptor M4 CHRM4 0.1509
274 Muscarinic acetylcholine receptor M5 CHRM5 0.1215
3923 Cholinesterase BCHE 0.1171
1193 Proteinase-activated receptor 1 F2R 0.0777
4512 Cytochrome P450 3A4 CYP3A4 0.0749
4119 Cytochrome P450 2D6 CYP2D6 0.071
492 Histamine H1 receptor HRH1 0.0639
1588 Multidrug resistance protein 1 ABCB1 0.0563
6145 Solute carrier family 22 member 1 SLC22A1 0.0508
474 Acetylcholinesterase ACHE 0.0491
234 Plasminogen PLG 0.0448
232 Corticosteroid-binding globulin SERPINA6 0.0432
341 5-hydroxytryptamine 3 receptor HTR3A 0.0426
6144 Solute carrier family 22 member 2 SLC22A2 0.0373
502 5-hydroxytryptamine 2A receptor HTR2A 0.0368
871 Glucocorticoid receptor NR3C1 0.0368
588 Chromodomain-helicase-DNA-binding protein 1 CHD1 0.033
831 D(2) dopamine receptor DRD2 0.0329
6020 Aldehyde oxidase AOX1 0.0319
1729 Solute carrier family 22 member 6 SLC22A6 0.0315
6116 Gastric triacylglycerol lipase LIPF 0.0301
1757 Myeloperoxidase MPO 0.0301
556 Alpha-1A adrenergic receptor ADRA1A 0.0292
4118 Cytochrome P450 3A5 CYP3A5 0.0287
1295 Fatty acid synthase FASN 0.028
6013 Cytochrome P450 2E1 CYP2E1 0.0271
754 Pancreatic triacylglycerol lipase PNLIP 0.0268
3823 Cytokine receptor common gamma chain IL2RG 0.0254
23 D(1A) dopamine receptor DRD1 0.0251
590 5-hydroxytryptamine 2C receptor HTR2C 0.0237
706 Glutamate [NMDA] receptor subunit 3A GRIN3A 0.0235
6016 Cytochrome P450 2C19 CYP2C19 0.0227
4132 Chloride channel protein ClC-Ka CLCNKA 0.0225
724 Interleukin-2 receptor alpha chain IL2RA 0.0221
717 Interleukin-2 receptor subunit beta IL2RB 0.0221
824 Sodium-dependent serotonin transporter SLC6A4 0.0215
1770 Phospholipase C PLCL1 0.0206
2841 Phospholipase C plc 0.0206
1759 85 kDa calcium-independent phospholipase A2 PLA2G6 0.0206
4165 P2Y purinoceptor 2 P2RY2 0.0198
4757 Cytochrome P450 2C9 CYP2C9 0.0198
540 Sodium-dependent noradrenaline transporter SLC6A2 0.0196
4200 Cytochrome P450 1A2 CYP1A2 0.0181
430 Follicle-stimulating hormone receptor FSHR 0.0179
713 Sodium-dependent dopamine transporter SLC6A3 0.0177
290 Prostaglandin G/H synthase 2 PTGS2 0.0177
817 DNA topoisomerase 2-alpha TOP2A 0.0173
6178 UDP-glucuronosyltransferase 2B7 UGT2B7 0.0165
2654 Complement control protein C3L 0.0161
1181 Alpha-1-acid glycoprotein 1 ORM1 0.0161
6107 Cytochrome P450 3A7 CYP3A7 0.0161
4924 Cytochrome P450 2C8 CYP2C8 0.0159
789 Alpha-1D adrenergic receptor ADRA1D 0.0159
6030 Cytochrome P450 2B6 CYP2B6 0.0155
833 Organic cation/carnitine transporter 1 SLC22A4 0.0155
458 Neuronal acetylcholine receptor subunit alpha-10 CHRNA10 0.0154
5766 NAD-dependent deacetylase sirtuin-5 SIRT5 0.0154
632 Alpha-1B adrenergic receptor ADRA1B 0.0147
862 Multidrug resistance-associated protein 1 ABCC1 0.0147
5455 Arylsulfatase A ARSA 0.0146
814 Ryanodine receptor 1 RYR1 0.0146
4203 Histamine N-methyltransferase HNMT 0.0143
6500 Phospholipase A2 PLA2G1B 0.0141
489 Monocarboxylate transporter 2 SLC16A7 0.0137
320 5-hydroxytryptamine 1A receptor HTR1A 0.0136
432 D(4) dopamine receptor DRD4 0.0133
737 Mineralocorticoid receptor NR3C2 0.013
436 5-hydroxytryptamine 2B receptor HTR2B 0.0129
6024 Cytochrome P450 1A1 CYP1A1 0.0125
198 Sodium channel protein type 10 subunit alpha SCN10A 0.0124
118 Organic cation/carnitine transporter 2 SLC22A5 0.0124
124 Histamine H2 receptor HRH2 0.0122
6139 Solute carrier organic anion transporter family member 1A2 SLCO1A2 0.0121
2981 Phospholipase A2, membrane associated PLA2G2A 0.0119
614 Progesterone receptor PGR 0.0117
738 Monocarboxylate transporter 1 SLC16A1 0.0112
3947 Xanthine dehydrogenase/oxidase XDH 0.011
638 D(3) dopamine receptor DRD3 0.0109
318 Alpha-2A adrenergic receptor ADRA2A 0.0107
6018 UDP-glucuronosyltransferase 1-9 UGT1A9 0.0106
6098 Potassium voltage-gated channel subfamily D member 2 KCND2 0.0099
6099 Potassium voltage-gated channel subfamily D member 3 KCND3 0.0099
20 Prostaglandin G/H synthase 1 PTGS1 0.0097
5878 Alpha-7 nicotinic cholinergic receptor subunit CHRFAM7A 0.0096
2129 Sucrase-isomaltase, intestinal SI 0.0094
378 Alpha-2C adrenergic receptor ADRA2C 0.0092
6082 Neuronal acetylcholine receptor subunit beta-3 CHRNB3 0.0092
6080 Neuronal acetylcholine receptor subunit alpha-5 CHRNA5 0.0092
948 Neuronal acetylcholine receptor subunit beta-2 CHRNB2 0.0091
629 Alpha-2B adrenergic receptor ADRA2B 0.0091
5718 Cytochrome P450 2A6 CYP2A6 0.0087
1656 CYP2B protein CYP2B 0.0087
6081 Neuronal acetylcholine receptor subunit alpha-6 CHRNA6 0.0085
528 5-hydroxytryptamine 1E receptor HTR1E 0.0083
54 Prothrombin F2 0.0081
4097 Neuronal acetylcholine receptor subunit alpha-9 CHRNA9 0.0081
6078 Neuronal acetylcholine receptor subunit beta-4 CHRNB4 0.0078
1256 5-hydroxytryptamine 6 receptor HTR6 0.0077
163 D(1B) dopamine receptor DRD5 0.0075
6079 Neuronal acetylcholine receptor subunit alpha-3 CHRNA3 0.0071
716 5-hydroxytryptamine 7 receptor HTR7 0.007
220 Sodium channel protein type 5 subunit alpha SCN5A 0.0065
725 5-hydroxytryptamine 1D receptor HTR1D 0.0062
885 5-hydroxytryptamine 1B receptor HTR1B 0.0061
319 Opioid receptor, sigma 1 OPRS1 0.006
6176 UDP-glucuronosyltransferase 1-3 UGT1A3 0.0059
947 Neuronal acetylcholine receptor subunit alpha-4 CHRNA4 0.0058
6104 Dimethylaniline monooxygenase [N-oxide-forming] 1 FMO1 0.0053
4095 Neuronal acetylcholine receptor subunit alpha-7 CHRNA7 0.0053
174 Sigma 1-type opioid receptor SIGMAR1 0.0048
465 Calmodulin CALM1 0.0047
215 Sodium channel protein type 11 subunit alpha SCN11A 0.0045
6147 Solute carrier family 22 member 3 SLC22A3 0.0044
6432 Transporter snf 0.0039
94 5-hydroxytryptamine 4 receptor HTR4 0.0036
3941 Amine oxidase [flavin-containing] A MAOA 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
587 Serum albumin ALB 0.003
805 Cytochrome P450 11B1, mitochondrial CYP11B1 0.0029
6106 Cytochrome P450 2C18 CYP2C18 0.0028
1360 Sphingomyelin phosphodiesterase SMPD1 0.0027
6101 Dimethylaniline monooxygenase [N-oxide-forming] 3 FMO3 0.0027
6014 Cytochrome P450 2A13 CYP2A13 0.0026
6047 Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A PDE1A 0.0025
6100 BDNF/NT-3 growth factors receptor NTRK2 0.0024
5692 Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B PDE1B 0.0024
762 Voltage-dependent calcium channel subunit alpha-2/delta-1 CACNA2D1 0.0019
4110 Voltage-dependent L-type calcium channel subunit beta-2 CACNB2 0.0019
4115 Voltage-dependent L-type calcium channel subunit alpha-1D CACNA1D 0.0019
1618 High affinity nerve growth factor receptor NTRK1 0.0019
478 Voltage-dependent L-type calcium channel subunit alpha-1C CACNA1C 0.0018
1086 Potassium voltage-gated channel subfamily KQT member 2 KCNQ2 0.0018
164 Histamine H4 receptor HRH4 0.0017
3939 Amine oxidase [flavin-containing] B MAOB 0.0016
734 D1 dopamine receptor-interacting protein calcyon CALY 0.0016
872 Gamma-aminobutyric-acid receptor subunit alpha-1 GABRA1 0.0015
858 Potassium voltage-gated channel subfamily A member 1 KCNA1 0.0015
193 Beta-1 adrenergic receptor ADRB1 0.0013
766 Beta-2 adrenergic receptor ADRB2 0.0012
6025 UDP-glucuronosyltransferase 1-4 UGT1A4 0.0012
467 Delta-type opioid receptor OPRD1 0.0012
696 Kappa-type opioid receptor OPRK1 0.0012
1898 Cytochrome P450 1B1 CYP1B1 0.001
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