Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMP6M1N)

• Drug Name: Pirenzepine Drug Info
• Synonyms: Gasteril; Gastrotsepin; Gastrozepin; Pirenzepin; Pirenzepina; Pirenzepinum; Pyrenzepine; Ulcosan; Pirenzepine Gastrozepin; Gastrozepin (TN); L-S 519; Pirenzepina [INN-Spanish]; Pirenzepine (INN); Pirenzepine [INN:BAN]; Pirenzepinum [INN-Latin]; 11-((4-Methyl-1-piperazinyl)acetyl)-5,11-dihydro-6H-pyrido(2,3-b)(1,4)benzodiazepin-6-one; 11-[(4-methylpiperazin-1-yl)acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one; 11-[2-(4-methylpiperazin-1-yl)acetyl]-5H-pyrido[2,3-b][1,4]benzodiazepin-6-one; 5,11-Dihydro-11-((4-methyl-1-piperazinyl)acetyl)-6H-pyrido(2,3-b)(1,4)benzodiazepin-6-one

Indication

Disease Entry	ICD 11	Status	REF
Peptic ulcer	DA61	Approved	[1]

• Therapeutic Class: Antiulcer Agents
• Cross-matching ID:
  PubChem CID: 4848
  ChEBI ID: CHEBI:8247
  CAS Number: CAS 28797-61-7
  TTD Drug ID: DMP6M1N
  VARIDT Drug ID: DR01428

Molecule-Related Drug Atlas

Drug(s) Targeting Muscarinic acetylcholine receptor M1 (CHRM1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
ACECLIDINE	DMOLNCZ	Glaucoma/ocular hypertension	9C61	Approved	[5]
Fesoterodine fumarate	DM13495	Overactive bladder	GC50.0	Approved	[6]
SMT-D002	DM1I93C	Seborrhea	ED91.2	Approved	[7]
Clidinium	DMUMQZ0	Abdominal stomach pain	DD91.4	Approved	[8]
Trihexyphenidyl	DMB19L8	Dystonia	8A02	Approved	[9]
Oxyphenonium	DMMQHOZ	Visceral spasms	MD81.4	Approved	[10]
Benztropine	DMGZOVN	Parkinson disease	8A00.0	Approved	[11]
Glycopyrrolate	DM2M3ZA	Anaesthesia	9A78.6	Approved	[12]
Cycrimine	DM8C43Q	Parkinson disease	8A00.0	Approved	[13]
Dicyclomine	DMZSDGX	Functional bowel syndrome	DD91.0	Approved	[14]
Gabapentin	DM6T924	Complex partial seizure	8A68.0	Approved	[22]
Marinol	DM70IK5	Anorexia nervosa cachexia	6B80	Approved	[23]
Acetylcholine	DMDF79Z	Cataract	9B10	Approved	[24]
Atropine	DMEN6X7	Organophosphate poisoning	NE6Z	Approved	[25]
Clozapine	DMFC71L	Schizophrenia	6A20	Approved	[26]
Olanzapine	DMPFN6Y	Bipolar depression		Approved	[27]
Gallamine Triethiodide	DMPO0MS	Stabilize muscle contraction	FB3Z	Approved	[28]
Carbachol	DMX9K8F	Glaucoma/ocular hypertension	9C61	Approved	[24]
Methylscopolamine	DM5VWOB	Peptic ulcer	DA61	Approved	[29]
Dihydrotestosterone	DM3S8XC	Prostate hyperplasia	GA90	Phase 4	[30]

Drug(s) Transported By P-glycoprotein 1 (ABCB1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Amoxicillin	DMUYNEI	Acute otitis media	AB00	Approved	[15]
Doxorubicin	DMVP5YE	Acute myelogenous leukaemia	2A41	Approved	[16]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[17]
Folic Acid	DMEMBJC	Colorectal carcinoma		Approved	[18]
Fluorouracil	DMUM7HZ	Adenocarcinoma	2D40	Approved	[17]
Cisplatin	DMRHGI9	Adenocarcinoma	2D40	Approved	[17]
Progesterone	DMUY35B	Amenorrhea	GA20.0	Approved	[19]
Tamoxifen	DMLB0EZ	Breast cancer	2C60-2C65	Approved	[17]
Estradiol	DMUNTE3	Acne vulgaris	ED80	Approved	[20]
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[21]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Muscarinic acetylcholine receptor M1 (CHRM1)	TTZ9SOR	ACM1_HUMAN	Antagonist	[2]

Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	MOA	REF
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_HUMAN	Substrate	[3]

Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
Muscarinic acetylcholine receptor M1 (CHRM1)	OTKW3E6B	ACM1_HUMAN	Protein Interaction/Cellular Processes	[4]

References

• [1] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 328).
• [2] Negative crosstalk between M1 and M2 muscarinic autoreceptors involves endogenous adenosine activating A1 receptors at the rat motor endplate. Neurosci Lett. 2009 Aug 14;459(3):127-31.
• [3] Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs. J Pharmacol Exp Ther. 2002 Dec;303(3):1029-37.
• [4] Fluorescent pirenzepine derivatives as potential bitopic ligands of the human M1 muscarinic receptor. J Med Chem. 2004 Aug 12;47(17):4300-15. doi: 10.1021/jm040800a.
• [5] Design, synthesis, and neurochemical evaluation of 5-(3-alkyl-1,2,4- oxadiazol-5-yl)-1,4,5,6-tetrahydropyrimidines as M1 muscarinic receptor agonists. J Med Chem. 1993 Apr 2;36(7):842-7.
• [6] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [7] Demonstration of bladder selective muscarinic receptor binding by intravesical oxybutynin to treat overactive bladder. J Urol. 2004 Nov;172(5 Pt 1):2059-64.
• [8] Accidental acute clidinium toxicity. Emerg Med J. 2009 Jun;26(6):460.
• [9] The role of M1 muscarinic cholinergic receptors in the discriminative stimulus properties of N-desmethylclozapine and the atypical antipsychotic dr... Psychopharmacology (Berl). 2009 Apr;203(2):295-301.
• [10] Ultraviolet spectroscopic estimation of microenvironments and bitter tastes of oxyphenonium bromide in cyclodextrin solutions. J Pharm Sci. 1999 Aug;88(8):759-62.
• [11] Formulation and biopharmaceutical evaluation of transdermal patch containing benztropine. Int J Pharm. 2008 Jun 5;357(1-2):55-60.
• [12] Autonomic cardiovascular control during a novel pharmacologic alternative to ganglionic blockade. Clin Pharmacol Ther. 2008 May;83(5):692-701.
• [13] Capillary gas chromatography of trihexyphenidyl, procyclidine and cycrimine in biological fluids. J Chromatogr. 1989 Sep 29;494:135-42.
• [14] [Characterization of muscarinic receptors in undifferentiated thyroid cells in Fisher rats]. Endocrinol Nutr. 2009 Mar;56(3):106-11.
• [15] Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
• [16] MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
• [17] Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade. Cancer Lett. 2016 Jan 1;370(1):153-64.
• [18] Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
• [19] Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
• [20] Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
• [21] Association of genetic polymorphisms in the influx transporter SLCO1B3 and the efflux transporter ABCB1 with imatinib pharmacokinetics in patients with chronic myeloid leukemia. Ther Drug Monit. 2011 Apr;33(2):244-50.
• [22] ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
• [23] Evaluation of first generation synthetic cannabinoids on binding at non-cannabinoid receptors and in a battery of in?vivo assays in mice. Neuropharmacology. 2016 Nov;110(Pt A):143-153. doi: 10.1016/j.neuropharm.2016.07.016. Epub 2016 Jul 20.
• [24] Regional differences in functional receptor distribution and calcium mobilization in the intact human lens. Invest Ophthalmol Vis Sci. 2001 Sep;42(10):2355-63.
• [25] Assessment of false transmitters as treatments for nerve agent poisoning. Toxicol Lett. 2020 Mar 15;321:21-31. doi: 10.1016/j.toxlet.2019.12.010. Epub 2019 Dec 9.
• [26] Increasing D2 affinity results in the loss of clozapine's atypical antipsychotic action. Neuroreport. 2002 May 7;13(6):831-5. doi: 10.1097/00001756-200205070-00019.
• [27] No evidence for binding of clozapine, olanzapine and/or haloperidol to selected receptors involved in body weight regulation. Pharmacogenomics J. 2007 Aug;7(4):275-81. doi: 10.1038/sj.tpj.6500418. Epub 2006 Sep 19.
• [28] Allosteric interactions of staurosporine and other indolocarbazoles with N-[methyl-(3)H]scopolamine and acetylcholine at muscarinic receptor subtypes: identification of a second allosteric site. Mol Pharmacol. 2000 Jul;58(1):194-207.
• [29] Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors. Mol Pharmacol. 1997 Jul;52(1):172-9.
• [30] Androgen receptor-mediated repression of novel target genes. Prostate. 2007 Sep 15;67(13):1371-83. doi: 10.1002/pros.20623.