1227675-51-5

1227675-51-5 structure

Name: SCH 39166 hydrobromide
Chemical Name: (6aS,13bR)-11-Chloro-7-methyl-6,6a,7,8,9,13b-hexahydro-5H-benzo[d]naphtho[2,1-b]azepin-12-ol hydrobromide (1:1)
CAS Number: 1227675-51-5
Molecular Formula: C₁₉H₂₁BrClNO
Molecular Weight: 394.73
Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
Create Date: 2018-06-10 16:28:29
Modify Date: 2024-01-15 00:10:19
SCH 39166 hydrobromide (SCH391660) is potent and selective antagonist of dopamine D1/D5 receptor, with Kis of 1.2 nM and 2.0 nM, respectively. SCH 39166 hydrobromide shows more than 40-flod selectivity over D2, D4, 5-HT, and α2a receptor (Ki=0.98, 5.52, 0.08, and 0.73 μM, respectively). SCH 39166 hydrobromide can be used for the research of schizophrenia, cocaine addition, and obesity[1].

Name	(6aS,13bR)-11-Chloro-7-methyl-6,6a,7,8,9,13b-hexahydro-5H-benzo[d]naphtho[2,1-b]azepin-12-ol hydrobromide (1:1)
Synonyms	5H-Benzo[d]naphth[2,1-b]azepin-12-ol, 11-chloro-6,6a,7,8,9,13b-hexahydro-7-methyl-, (6aS,13bR)-, hydrobromide (1:1) (6aS,13bR)-11-Chloro-7-methyl-6,6a,7,8,9,13b-hexahydro-5H-benzo[d]naphtho[2,1-b]azepin-12-ol hydrobromide (1:1) SCH39166

Description	SCH 39166 hydrobromide (SCH391660) is potent and selective antagonist of dopamine D1/D5 receptor, with Kis of 1.2 nM and 2.0 nM, respectively. SCH 39166 hydrobromide shows more than 40-flod selectivity over D2, D4, 5-HT, and α2a receptor (Ki=0.98, 5.52, 0.08, and 0.73 μM, respectively). SCH 39166 hydrobromide can be used for the research of schizophrenia, cocaine addition, and obesity[1].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor Research Areas >> Metabolic Disease Research Areas >> Neurological Disease Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor
Target	D1 Receptor:1.2 nM (Ki) D5 Receptor:2.0 nM (Ki) D2 Receptor:980 nM (Ki) D4 Receptor:5520 nM (Ki) 5-HT Receptor:80 nM (Ki) Alpha-2A adrenergic receptor:731 nM (Ki)
In Vitro	SCH 39166 (2 μM) hydrobromide completely abolishes the proconvulsive effect of Dopamine (10 μM) in isolated corticohippocampal formation[2].
In Vivo	SCH 39166 (0.003-0.3 mg/kg; a single s.c.) hydrobromide abolishes Nicotine-induced enhancement of a sensory reinforcer in adult rats[3]. Animal Model: Male young adult Long-Evans rats were injected with Nicotine[3] Dosage: 0.003, 0.01, 0.03, 0.1, 0.3 mg/kg Administration: A single s.c. 20 min before Nicotine (0.1 mg/kg) Result: Dose-dependently reduced pressing on both active and inactive levers.
References	[1]. Wu WL, et, al. Dopamine D1/D5 receptor antagonists with improved pharmacokinetics: design, synthesis, and biological evaluation of phenol bioisosteric analogues of benzazepine D1/D5 antagonists. J Med Chem. 2005 Feb 10;48(3):680-93. [2]. Sharopov S, et, al. Dopaminergic modulation of low-Mg²⁺-induced epileptiform activity in the intact hippocampus of the newborn mouse in vitro. J Neurosci Res. 2012 Oct;90(10):2020-33. [3]. Satanove DJ, et, al. Nicotine-induced enhancement of a sensory reinforcer in adult rats: antagonist pretreatment effects. Psychopharmacology (Berl). 2021 Feb;238(2):475-486.

Molecular Formula	C₁₉H₂₁BrClNO
Molecular Weight	394.73
Exact Mass	393.049500

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