(6AS-TRANS)-11-CHLORO-6,6A,7,8,9,13B-HEXAHYDRO-7-METHYL-5H-BENZO[D]NAPHTH[2,1-B]AZEPIN-12-OL HYDROBROMIDE Chemical Properties

storage temp. 

Desiccate at RT

solubility 

DMSO: Slightly Soluble; Methanol: Slightly Soluble; Water: Slightly Soluble

form 

A solid

Stability:

Hygroscopic

(6AS-TRANS)-11-CHLORO-6,6A,7,8,9,13B-HEXAHYDRO-7-METHYL-5H-BENZO[D]NAPHTH[2,1-B]AZEPIN-12-OL HYDROBROMIDE Usage And Synthesis

Description

SCH 39166 is a dopamine D₁ receptor antagonist (K_i = 5 nM). It is selective for D₁ over D_2-4 receptors (K_is = 3,751, >1,000, and 5,934 nM, respectively), however, it also binds to D₅ receptors (K_i = 4.4 nM). SCH 39166 inhibits food intake in a dose-dependent manner in rats (ED₅₀ = 0.84 mg/kg). It reduces ethanol intake in Sardinian alcohol-preferring rats and sucrose intake in water-deprived and water-sated rats without affecting food or total fluid intake. SCH 39166 also suppresses cocaine-induced arrhythmias in anesthetized dogs.

Uses

SCH 39166 is a dopamine D1/D5 receptor antagonist used in the treatment of schizophrenia, cocaine addiction and obesity.

storage

Desiccate at RT

References

[1] M.A.B. TICE. Characterization of the binding of SCH 39166 to the five cloned dopamine receptor subtypes[J]. Pharmacology Biochemistry and Behavior, 1994, 49 3: Pages 567-571. DOI: 10.1016/0091-3057(94)90070-1
[2] P TERRY  J L K. A comparison of the effects of the D1 receptor antagonists SCH 23390 and SCH 39166 on suppression of feeding behavior by the D1 agonist SKF38393.[J]. Psychopharmacology, 1994, 113 3-4: 328-333. DOI: 10.1007/bf02245205
[3] I PANOCKA. Effects of the dopamine D1 receptor antagonist SCH 39166 on the ingestive behaviour of alcohol-preferring rats.[J]. Psychopharmacology, 1995, 120 2: 227-235. DOI: 10.1007/bf02246198
[4] P M KANANI. Acute deleterious effects of cocaine on cardiac conduction, hemodynamics, and ventricular fibrillation threshold: effects of interaction with a selective dopamine D1 antagonist SCH 39166.[J]. Journal of Cardiovascular Pharmacology, 1998, 32 1: 42-48. DOI: 10.1097/00005344-199807000-00007