SCH 39166 hydrobromide

Names

[ Name ]:
SCH 39166 hydrobromide

[Synonym ]:
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

Biological Activity

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₉H₂₁BrClNO

[ Molecular Weight ]:
394.73

[ Exact Mass ]:
393.049500

Related Compounds

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