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

General Information of Drug (ID: DM6PVWS)

• Drug Name: Telenzepine Drug Info
• Synonyms: Telenzepine [INN]; Telenzepinum [Latin]; Telenzepino [Spanish]; 80880-90-6; UNII-0990EG3K10; 0990EG3K10; NCGC00015987-05; DSSTox_RID_80752; DSSTox_CID_25209; 1-methyl-10-[2-(4-methylpiperazin-1-yl)acetyl]-5H-thieno[3,4-b][1,5]benzodiazepin-4-one; DSSTox_GSID_45209; 4,9-Dihydro-3-methyl-4-((4-methyl-1-piperazinyl)acetyl)-10H-thieno(3,4-b)(1,5)benzodiazepin-10-one; Telenzepine hydrochloride; Telenzepine dihydrochloide; C19H22N4O2S; Telenzepino; Telenzepinum; Telenzepine dihydrochloride hydrate; BY-802; [3H](+)telenzepine

Indication

Disease Entry	ICD 11	Status	REF
Chronic obstructive pulmonary disease	CA22	Discontinued in Preregistration	[1]

• Cross-matching ID:
  PubChem CID: 5387
  ChEBI ID: CHEBI:92110
  CAS Number: CAS 80880-90-6
  TTD Drug ID: DM6PVWS

Molecule-Related Drug Atlas

Drug(s) Targeting Muscarinic acetylcholine receptor (CHRM)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Acetylcholine	DMDF79Z	Cataract	9B10	Approved	[4]
Tiotropium	DMFDC0Q	Chronic obstructive pulmonary disease	CA22	Approved	[5]
Darifenacin	DMWXLYZ	Overactive bladder	GC50.0	Approved	[6]
Methylscopolamine	DM5VWOB	Peptic ulcer	DA61	Approved	[7]
Clidinium	DMUMQZ0	Abdominal stomach pain	DD91.4	Approved	[8]
Oxybutynin hydrochloride	DMF2KLU	Urinary incontinence	MF50.2	Approved	[9]
Incruse Ellipta	DM32GSJ	Chronic obstructive pulmonary disease	CA22	Approved	[10]
Revefenacin	DMMP5SI	Chronic obstructive pulmonary disease	CA22	Approved	[11]
Scopolamine	DMOM8AL	Addictive disorder	6C50-6C5Z	Approved	[12]
Isopropamide iodide	DMQYV60	Allergic rhinitis	CA08.0	Approved	[13]

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	[14]
Fesoterodine fumarate	DM13495	Overactive bladder	GC50.0	Approved	[15]
SMT-D002	DM1I93C	Seborrhea	ED91.2	Approved	[16]
Clidinium	DMUMQZ0	Abdominal stomach pain	DD91.4	Approved	[17]
Trihexyphenidyl	DMB19L8	Dystonia	8A02	Approved	[18]
Oxyphenonium	DMMQHOZ	Visceral spasms	MD81.4	Approved	[19]
Benztropine	DMGZOVN	Parkinson disease	8A00.0	Approved	[20]
Glycopyrrolate	DM2M3ZA	Anaesthesia	9A78.6	Approved	[21]
Pirenzepine	DMP6M1N	Peptic ulcer	DA61	Approved	[22]
Cycrimine	DM8C43Q	Parkinson disease	8A00.0	Approved	[23]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Muscarinic acetylcholine receptor (CHRM)	TTOXS3C	NOUNIPROTAC	Antagonist	[2]
Muscarinic acetylcholine receptor M1 (CHRM1)	TTZ9SOR	ACM1_HUMAN	Modulator	[3]

References

• [1] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000603)
• [2] The existence of stable enantiomers of telenzepine and their stereoselective interaction with muscarinic receptor subtypes. Mol Pharmacol. 1989 Apr;35(4):477-83.
• [3] Effect of telenzepine, an M1-selective muscarinic receptor antagonist, in patients with nocturnal asthma. Pulm Pharmacol. 1994 Apr;7(2):91-7.
• [4] Thiochrome enhances acetylcholine affinity at muscarinic M4 receptors: receptor subtype selectivity via cooperativity rather than affinity. Mol Pharmacol. 2004 Jan;65(1):257-66.
• [5] Pharmacological characterization of GSK573719 (umeclidinium): a novel, long-acting, inhaled antagonist of the muscarinic cholinergic receptors for treatment of pulmonary diseases. J Pharmacol Exp Ther. 2013 May;345(2):260-70.
• [6] Characterisation of [3H]-darifenacin as a novel radioligand for the study of muscarinic M3 receptors. J Recept Signal Transduct Res. 1997 Jan-May;17(1-3):177-84.
• [7] Lithocholylcholine, a bile acid/acetylcholine hybrid, is a muscarinic receptor antagonist. J Pharmacol Exp Ther. 2002 Oct;303(1):29-35.
• [8] Pharmacological comparison of the cloned human and rat M2 muscarinic receptor genes expressed in the murine fibroblast (B82) cell line. J Pharmacol Exp Ther. 1998 Feb;284(2):500-7.
• [9] Effects of propiverine hydrochloride (propiverine) on the muscarinic receptor binding affinity in guinea pig tissues and on salivation in conscious dogs. Nihon Yakurigaku Zasshi. 1999 Mar;113(3):157-66.
• [10] Clinical pipeline report, company report or official report of GlaxoSmithKline.
• [11] 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
• [12] The amygdala modulates morphine-induced state-dependent memory retrieval via muscarinic acetylcholine receptors. Neuroscience. 2009 May 5;160(2):255-63.
• [13] 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.
• [14] 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.
• [15] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [16] Demonstration of bladder selective muscarinic receptor binding by intravesical oxybutynin to treat overactive bladder. J Urol. 2004 Nov;172(5 Pt 1):2059-64.
• [17] Accidental acute clidinium toxicity. Emerg Med J. 2009 Jun;26(6):460.
• [18] 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.
• [19] Ultraviolet spectroscopic estimation of microenvironments and bitter tastes of oxyphenonium bromide in cyclodextrin solutions. J Pharm Sci. 1999 Aug;88(8):759-62.
• [20] Formulation and biopharmaceutical evaluation of transdermal patch containing benztropine. Int J Pharm. 2008 Jun 5;357(1-2):55-60.
• [21] Autonomic cardiovascular control during a novel pharmacologic alternative to ganglionic blockade. Clin Pharmacol Ther. 2008 May;83(5):692-701.
• [22] 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.
• [23] Capillary gas chromatography of trihexyphenidyl, procyclidine and cycrimine in biological fluids. J Chromatogr. 1989 Sep 29;494:135-42.