A positive allosteric modulator of GABAB receptors; enhances GABA binding with a maximal effect of 143% compared to a GABA-only control in CHO cells membranes expressing the GABAB(1b/2) receptor and enhances GABA binding to rat cortical membranes at 30 µM; selective for GABA binding to heterodimeric GABAB(1b/2) over monomeric GABAB(1b) receptors; potentiates the efficacy of baclofen in decreasing the spontaneous firing rate of dopaminergic neurons in the rat VTA in vitro (EC50 = 0.27 µM); also potentiates the sedative-reducing effects induced by baclofen or GHB in rats at 10-170 mg/kg; suppresses the acquisition of alcohol drinking behavior in alcohol-naïve Sardinian alcohol-preferring rats over a five-day period at 25-100 mg/kg and transiently reduces the maintenance of alcohol drinking behavior in alcohol-experienced rats at a dose of 100 mg/kg

CGP 7930 – 10 mg

Brand:
Cayman
CAS:
57717-80-3
Storage:
-20
UN-No:
Non-Hazardous - /

CGP 7930 is a positive allosteric modulator of GABAB receptors.{45680} It enhances GABA binding with a maximal effect of 143% compared to a GABA-only control in CHO cells membranes expressing the GABAB(1b/2) receptor and enhances GABA binding to rat cortical membranes when used at a concentration of 30 µM. It is selective for GABA binding to heterodimeric GABAB(1b/2) over monomeric GABAB(1b) receptors. CGP 7930 potentiates the efficacy of the GABAB receptor agonist baclofen (Item No. 27326) in decreasing the spontaneous firing rate of dopaminergic neurons in the rat ventral tegmental area (VTA) in vitro (EC50 = 0.27 µM).{45681} It also potentiates the sedative-reducing effects induced by the GABAB receptor agonists baclofen and γ-hydroxybutyric acid (GHB) in rats when administered at doses ranging from 10 to 170 mg/kg, effects that can be blocked by the GABAB receptor antagonist SCH 50911.{45682} CGP 7930 reduces self-administration of nicotine, alcohol, and cocaine in rodent models.{45683} It suppresses the acquisition of alcohol drinking behavior in alcohol-naïve Sardinian alcohol-preferring rats over a five-day period when administered at doses ranging from 25 to 100 mg/kg and transiently reduces the maintenance of alcohol drinking behavior in alcohol-experienced rats at a dose of 100 mg/kg.{45684}  

 

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Description

A positive allosteric modulator of GABAB receptors; enhances GABA binding with a maximal effect of 143% compared to a GABA-only control in CHO cells membranes expressing the GABAB(1b/2) receptor and enhances GABA binding to rat cortical membranes at 30 µM; selective for GABA binding to heterodimeric GABAB(1b/2) over monomeric GABAB(1b) receptors; potentiates the efficacy of baclofen in decreasing the spontaneous firing rate of dopaminergic neurons in the rat VTA in vitro (EC50 = 0.27 µM); also potentiates the sedative-reducing effects induced by baclofen or GHB in rats at 10-170 mg/kg; suppresses the acquisition of alcohol drinking behavior in alcohol-naïve Sardinian alcohol-preferring rats over a five-day period at 25-100 mg/kg and transiently reduces the maintenance of alcohol drinking behavior in alcohol-experienced rats at a dose of 100 mg/kg

Formal name: 3,5-bis(1,1-dimethylethyl)-4-hydroxy-β,β-dimethyl-benzenepropanol

Synonyms: 

Molecular weight: 292.5

CAS: 57717-80-3

Purity: ≥98%

Formulation: A crystalline solid

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