A D1 and D5 receptor partial agonist (Kis = 1.18 and 7.56 nM

SKF 83959 (hydrobromide) – 25 mg

Brand:
Cayman
CAS:
67287-95-0
Storage:
-20
UN-No:
Non-Hazardous - /

SKF 83959 is a partial agonist at the dopamine D1-like receptors (Kis = 1.18 and 7.56 nM, respectively, for D1 and D5) that is selective over the D2-like receptors (Kis = 920 and 399 nM, respectively, for D2 and D3).{24103,40094} It is protective against oxidative stress in retinal ganglion cells after hydrogen peroxide-induced injury in vitro.{40095} In a rat methylazoxymethanol acetate (MAM) model of schizophrenia, it had positive effects on hippocampal function, determined using electrophysiology, but impaired spatial learning.{40096} SKF 83959 can also act as an allosteric modulator of the sigma-1 (σ1) receptor by enhancing the binding to and delaying the dissociation of the selective σ1-receptor agonist pentazocine.{40097}  

 

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Description

A D1 and D5 receptor partial agonist (Kis = 1.18 and 7.56 nM, respectively, for D1 and D5); selective over the D2-like receptors (Kis = 920 and 399 nM, respectively, for D2 and D3); protective against oxidative stress in retinal ganglion cells; can also act as an allosteric modulator of the σ1 receptor

Formal name: 6-chloro-2,3,4,5-tetrahydro-3-methyl-1-(3-methylphenyl)-1H-3-benzazepine-7,8-diol, monohydrobromide

Synonyms: 

Molecular weight: 398.7

CAS: 67287-95-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Product Type|Biochemicals|Receptor Pharmacology|Allosteric Modulators||Research Area|Neuroscience|Behavioral Neuroscience|Schizophrenia & Psychosis||Research Area|Oxidative Stress & Reactive Species|Antioxidant Activity||Research Area|Oxidative Stress & Reactive Species|Reactive Oxygen

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