Telenzepine dihydrochloride - CAS 147416-96-4
Category: Inhibitor
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Molecular Formula:
C19H22N4O2S.2HCl
Molecular Weight:
443.39
COA:
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Targets:
mAChR
Description:
Telenzepine dihydrochloride is a selective and high affinity muscarinic M1 receptor antagonist (Ki = 0.94 nM). Telenzepine was demonstrated ability to inhibit gastric acid secretion.
Brife Description:
muscarinic M1 receptor antagonist
Related CAS:
80880-90-6 (free base)
Synonyms:
4,9-Dihydro-3-methyl-4-[(4-methyl-1-piperazinyl)acetyl]-10H-thieno[3,4-b][1,5]benzodiazepin-10-one dihydrochloride; Telenzepine hydrochloride; SR-01000075349
MSDS:
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InChIKey:
JTQJFSQQHGPLOX-UHFFFAOYSA-N
InChI:
InChI=1S/C19H22N4O2S.2ClH/c1-13-18-14(12-26-13)19(25)20-15-5-3-4-6-16(15)23(18)17(24)11-22-9-7-21(2)8-10-22;;/h3-6,12H,7-11H2,1-2H3,(H,20,25);2*1H
Canonical SMILES:
CC1=C2C(=CS1)C(=O)NC3=CC=CC=C3N2C(=O)CN4CCN(CC4)C.Cl.Cl
1.Muscarinic acetylcholine receptor-dependent induction of persistent synaptic enhancement in rat hippocampus in vivo.
Li S;Cullen WK;Anwyl R;Rowan MJ Neuroscience. 2007 Jan 19;144(2):754-61. Epub 2006 Nov 13.
Presynaptic terminal autoinhibitory muscarinic acetylcholine (ACh) receptors are predominantly of the M2/M4 subtypes and antagonists at these receptors may facilitate cognitive processes by increasing ACh release. The present study examined the ability of the M2/M4 muscarinic ACh receptor antagonist N,N'-bis [6-[[(2-methoxyphenyl)methyl]amino]hexyl]-1,8-octane diamine tetrahydrochloride (methoctramine) to induce and modulate synaptic plasticity in the CA1 area of the hippocampus in urethane-anesthetized rats. Both methoctramine and another M2/M4 antagonist, {11-[[2-[(diethylamino)methyl]-1-piperidinyl]acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one} (AF-DX 116), caused a rapid onset and persistent increase in baseline synaptic transmission after i.c.v. injection. Consistent with a requirement for activation of non-M2 receptors by endogenously released ACh, the M1/M3 receptor selective antagonists 4-diphenylacetoxy-N-methylpiperidine methiodide (4-DAMP) and 4,9-dihydro-3-methyl-4-[(4-methyl-1-piperazinyl)acetyl]-10H-thieno[3,4-b][1,5]benzodiazepin-10-one dihydrochloride (telenzepine) prevented the induction of the persistent synaptic enhancement by methoctramine. The requirement for cholinergic activation was transient and independent of nicotinic ACh receptor stimulation.
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CAS 147416-96-4 Telenzepine dihydrochloride

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