Shanghai Nianxing Industrial Co., Ltd
China
Product Name: Clocapramine
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Purity: 98.0%
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Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: clocapramine
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Purity: 98.0%
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47739-98-0

47739-98-0 structure

47739-98-0 structure

Name: Clocapramine
Chemical Name: 1-[3-(2-chloro-5,6-dihydrobenzo[b][1]benzazepin-11-yl)propyl]-4-piperidin-1-ylpiperidine-4-carboxamide
CAS Number: 47739-98-0
Molecular Formula: C₂₈H₃₇ClN₄O
Molecular Weight: 481.07300
Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
Create Date: 2016-10-18 22:17:18
Modify Date: 2024-01-09 17:34:33
Clocapramine is an antagonist of the D2, 5-HT2A receptors.

Name	1-[3-(2-chloro-5,6-dihydrobenzo[b][1]benzazepin-11-yl)propyl]-4-piperidin-1-ylpiperidine-4-carboxamide
Synonyms	1'-[3-(3-chloro-10,11-dihydro-dibenzo[b,f]azepin-5-yl)-propyl]-octahydro-[1,4']bipyridinyl-4'-carboxylic acid amide 3-Chlorocarpipramine Clocapramine [INN] Clocapraminum Clocapramine HCl clocapramine Clocapramina

Description	Clocapramine is an antagonist of the D2, 5-HT2A receptors.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor Research Areas >> Neurological Disease
Target	D2 and 5-HT2A receptor[1]
In Vitro	Clocapramine has a moderate affinity for D2-receptors in vitro. Clocapramine shows higher affinity for 5-HT2A than for D2-receptors in vitro[1].
In Vivo	Clocapramine shows the lowest potency for D2-occupancy in vivo[1]. An in vivo receptor binding technique is used to evaluate the binding profiles of typical and atypical antipsychotic drugs to striatal dopamine-D2 and frontal serotonin-5-HT2 receptors in a rat brain using more specific ligands. Clocapramine produces ratios of potency in occupying 5-HT2 versus D2 receptors that fall between these two groups (ED50 of 14.5 mg/kg for D2, 4.9 mg/kg for 5-HT2)[2].
Animal Admin	Rats[2] Male Wistar rats (210 to 240 g) are housed in a temperature-controlled room with a 12-hour dark/light cycle (lights on at 8:30) and have free access to food and water. For competition studies, rats are pretreated with an intraperitoneal injection of varying doses of antipsychotic drugs or the same volume (0.21 to 0.24 mL) of the corresponding vehicle (DMSO), 10 minutes prior to the injection of [3H]-YM-09151-2 or [3H]-ketanserin.
References	[1]. Schotte A, et al. In vitro receptor binding and in vivo receptor occupancy in rat and guinea pig brain: risperidone compared with antipsychotics hitherto used. Jpn J Pharmacol. 1995 Dec;69(4):399-412. [2]. Sumiyoshi T, et al. Atypicality of several antipsychotics on the basis of in vivo dopamine-D2 and serotonin-5HT2 receptor occupancy. Neuropsychopharmacology. 1995 Feb;12(1):57-64.

Density	1.195g/cm3
Boiling Point	662.1ºC at 760 mmHg
Molecular Formula	C₂₈H₃₇ClN₄O
Molecular Weight	481.07300
Flash Point	354.2ºC
Exact Mass	480.26600
PSA	53.80000
LogP	5.86310
Index of Refraction	1.602

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