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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/08/28 22:26:36」(JST)

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Telenzepine is a selective M1 antimuscarinic used in the treatment of peptic ulcers.^[1] Telenzepine is atropisomeric, in other words the molecule has a stereogenic C–N-axis; in neutral aqueous solution it displays a half-life for racemization of the order of 1000 years. The enantiomers have been resolved. The activity is related to the (+)-isomer which is about 500-fold more active as the (–)-isomer at muscarinic receptors in the rat cerebal cortex.^[2]

References

^ Eveleigh, P.; Hulme, E. C.; Schudt, C.; Birdsall, N. J. (1989). "The existence of stable enantiomers of telenzepine and their stereoselective interaction with muscarinic receptor subtypes". Molecular pharmacology 35 (4): 477–483. PMID 2704371.
^ Clayden, J.; Moran, W. J.; Edwards, P. J.; Laplante, S. R. (2009). "The Challenge of Atropisomerism in Drug Discovery". Angewandte Chemie International Edition 48 (35): 6398–6401. doi:10.1002/anie.200901719. PMID 19637174.

External links

Telenzepine is at least 25 times more potent than pirenzepine--a dose response and comparative secretory study in man, Gut., 1987 July; 28(7): 888–895

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1. COPDにおける抗コリン療法の役割 role of anticholinergic therapy in copd

English Journal

Rivastigmine improves isolation rearing-induced prepulse inhibition deficits via muscarinic acetylcholine receptors in mice.

Higashino K1, Ago Y1, Umeki T1, Hasebe S2, Onaka Y1, Hashimoto H1,3, Takuma K2,3, Matsuda T4.
Psychopharmacology.Psychopharmacology (Berl).2015 Oct 31. [Epub ahead of print]
RATIONALE: The acetylcholinesterase inhibitors donepezil, galantamine, and rivastigmine are used for the treatment of Alzheimer's disease. We previously demonstrated that donepezil and galantamine differentially affect isolation rearing-induced prepulse inhibition (PPI) deficits and that this might
PMID 26518025

Galantamine promotes adult hippocampal neurogenesis via M₁ muscarinic and α7 nicotinic receptors in mice.

Kita Y1, Ago Y1, Higashino K1, Asada K1, Takano E1, Takuma K1, Matsuda T1.
The international journal of neuropsychopharmacology / official scientific journal of the Collegium Internationale Neuropsychopharmacologicum (CINP).Int J Neuropsychopharmacol.2014 Dec;17(12):1957-68. doi: 10.1017/S1461145714000613. Epub 2014 May 12.
Galantamine, an inhibitor of acetylcholinesterase, promotes hippocampal neurogenesis, but the exact mechanism for this is not known. In the present study, we examined the mechanisms underlying the effects of acute galantamine on neurogenesis in the mouse hippocampus. Galantamine (3 mg/kg) increased
PMID 24818616

M1-muscarinic receptors promote fear memory consolidation via phospholipase C and the M-current.

Young MB1, Thomas SA.
The Journal of neuroscience : the official journal of the Society for Neuroscience.J Neurosci.2014 Jan 29;34(5):1570-8. doi: 10.1523/JNEUROSCI.1040-13.2014.
Neuromodulators released during and after a fearful experience promote the consolidation of long-term memory for that experience. Because overconsolidation may contribute to the recurrent and intrusive memories of post-traumatic stress disorder, neuromodulatory receptors provide a potential pharmaco
PMID 24478341

Japanese Journal

感覚情報処理機能障害に対するガランタミンの有効性とそのメカニズム

吾郷由希夫
YAKUGAKU ZASSHI 130(10), 1305-1310, 2010
… In addition, we unexpectedly found that the galantamine-induced improvements in PPI deficits were prevented by the muscarinic ACh receptor (mAChR) antagonists scopolamine and telenzepine (preferential for M1 subtype), but not by the nAChR antagonists. …
NAID 130000451673

Calcium Signaling and c-Fos Gene Expression via M_3 Muscarinic Acetylcholine Receptors in Human T-and B-Cells

FUJII Takeshi,KAWASHIMA Koichiro
The Japanese journal of pharmacology 84(2), 124-132, 2000-10-01
… with 100μM oxotremorine−M, an M1/M3 agonist, increased levels of intracellular free Ca2+([Ca2+]i)and c−fos mRNA expression in both cell lines.4−DAMP, an M3 antagonist, more effectively blocked the oxotremorine−M−induced increase in [Ca2+]i than pirenzepine and telenzepine, M1−receptor antagonists;AF−DX 116, an M2 antagonist;hexahydrosiladifenidol, a weak M3 antagonist;or hexamethonium and d−tubocurarine, nicotinic receptor antagonists.McN−A−343(100μM), a partial M1−receptor agonist, had no apparent effect on [Ca2+]i in either …
NAID 10008185481

Related Pictures

★リンクテーブル★

リンク元	「ムスカリン受容体拮抗薬」「テレンゼピン」

「ムスカリン受容体拮抗薬」

Telenzepine
Systematic (IUPAC) name
	1-methyl-10-[2-(4-methylpiperazin-1-yl)acetyl]-5H-thieno[3,4-b][1,5]benzodiazepin-4-one
Identifiers
CAS Registry Number	80880-90-6
ATC code	None
PubChem	CID: 5387
ChemSpider	5194
UNII	0990EG3K10
ChEMBL	CHEMBL253978
Chemical data
Formula	C19H22N4O2S
Molecular mass	370.47 g/mol
	SMILES CC1=C2C(=CS1)C(=O)NC3=CC=CC=C3N2C(=O)CN4CCN(CC4)C ;