CGP7930 - CAS 57717-80-3
Catalog number:
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
Molecular Weight:
GABA Receptor
CGP7930 is a positive allosteric modulator at the GABAB receptor. It has anxiolytic effects in animal studies, and has a synergistic effect with GABAB agonists such as baclofen and GHB. It increases the potency and efficacy of GABA at both native and recombinant GABAB receptors with EC50 values of 5.37 and 4.60μM respectively. It also enhances the inhibitory effect of the agonist L-baclofen in cultured cortical neurons. It reduces operant self-administration of ethanol and cocaine in rats.
Publictions citing BOC Sciences Products
  • >> More
>98 %
White solid
DMSO: 22 mg/mL, soluble
CGP7930 has anxiolytic effects in animal studies, and has a synergistic effect with GABAB agonists such as baclofen and GHB. It reduces operant self-administration of ethanol and cocaine in rats.
Quality Standard:
In-house standard
Grams to Kilograms
Boiling Point:
364.7±37.0 °C | Condition: Press: 760 Torr
Melting Point:
80-82 °C | Condition: Solv: hexane (110-54-3)
0.971±0.06 g/cm3 | Condition: Temp: 20 °C Press: 760 Torr
Canonical SMILES:
1.Effects of GABA(B) receptor antagonist, agonists and allosteric positive modulator on the cocaine-induced self-administration and drug discrimination.
Filip M1, Frankowska M, Przegaliński E. Eur J Pharmacol. 2007 Nov 28;574(2-3):148-57. Epub 2007 Jul 31.
Preclinical and clinical findings indicate that a GABA(B) receptor agonist baclofen decreases cocaine use. The present study investigated the effects of the GABA(B) receptor antagonist (2S)-(+)-5,5-dimethyl-2-morpholineacetic acid (SCH 50911), the agonists baclofen and 3-aminopropyl(methyl)phoshinic acid (SKF 97541) and the allosteric positive modulator 3,5-bis(1,1-dimethylethyl-4-hydroxy-beta,beta-dimethylbenzenepropanol (CGP 7930) in cocaine-and food-maintained responding under a fixed ratio 5 schedule of reinforcement in male Wistar rats. The effects of the GABA(B) receptor ligands on cocaine (10 mg/kg)-induced discriminative stimulus in a two-lever, water-reinforced fixed ratio 20 task and on basal locomotor activity were also assessed. Baclofen (2.5-5 mg/kg), SKF 97541 (0.1-0.3 mg/kg) and CGP 7930 (30-100 mg/kg) decreased the cocaine (0.5 mg/kg/injection)-maintained responding; SCH 50911 (3-10 mg/kg) was inactive in this respect. Baclofen (5 mg/kg) and SKF 97541 (0.
2.Effects of GABA(B) receptor agents on cocaine priming, discrete contextual cue and food induced relapses.
Filip M1, Frankowska M. Eur J Pharmacol. 2007 Oct 1;571(2-3):166-73. Epub 2007 Jun 13.
In the present study we investigated the effects of the GABA(B) receptor antagonist (2S)-(+)-5,5-dimethyl-2-morpholineacetic acid (SCH 50911), the agonists baclofen and 3-aminopropyl(methyl)phosphinic acid (SKF 97541), and the allosteric positive modulator 3,5-bis(1,1-dimethylethyl)-4-hydroxy-beta,beta-dimethylbenzenepropanol (CGP 7930) on cocaine seeking behavior. The effects of the above drugs on the reinstatement of responding induced by natural reinforcer (food) were also studied. Male Wistar rats were trained to self-administer either cocaine (0.5 mg/kg/infusion) or food (sweet milk) and responding on the reinforcer-paired lever was extinguished. Reinstatement of responding was induced by a noncontingent presentation of the self-administered reinforcer (10 mg/kg cocaine, i.p.), a discrete contextual cue, or a contingent presentation of food. SCH 50911 (3-10 mg/kg) dose-dependently attenuated responding on the previously cocaine-paired lever during both reinstatement conditions, with slightly greater efficacy at reducing conditioned cue reinstatement.
3.Effects of GABAB receptor ligands in animal tests of depression and anxiety.
Frankowska M1, Filip M, Przegaliński E. Pharmacol Rep. 2007 Nov-Dec;59(6):645-55.
Preclinical evidence strongly implicates GABA(B) receptors in the pathophysiology of several psychiatric disorders including anxiety and depression. In the present study, we investigated the effects of the selective GABA(B) receptor agonists baclofen and SKF 97541, the GABA(B) receptor positive allosteric modulator CGP7930 and the GABA(B) receptor antagonist SCH 50911 in the modified forced swimming test (FST) and in the elevated zero maze test (EZM), i.e. in animal models predictive of antidepressant and antianxiety activities, respectively. The classical antidepressant imipramine and the anxiolytic diazepam were employed as control drugs in the FST and in the EZM, respectively. In the FST, baclofen (0.25 mg/kg), SKF 97541 (0.01-0.05 mg/kg) or CGP 7930 (1-3 mg/kg) and SCH 50911 (1-3 mg/kg) showed antidepressant-like activity, significantly decreasing immobility time; these effects were not related to changes in locomotor activity. The antidepressant effects produced by the GABA(B) receptor ligands were compared with that of imipramine (30 mg/kg).
4.Effects of imipramine or GABA(B) receptor ligands on the immobility, swimming and climbing in the forced swim test in rats following discontinuation of cocaine self-administration.
Frankowska M1, Gołda A, Wydra K, Gruca P, Papp M, Filip M. Eur J Pharmacol. 2010 Feb 10;627(1-3):142-9. doi: 10.1016/j.ejphar.2009.10.049. Epub 2009 Oct 28.
We tested if discontinuation of cocaine self-administration can lead to the development of depressive-like symptoms in the forced swim test expressed as changes in immobility, swimming and climbing behaviors in rats. A "yoked" procedure in which rats were run simultaneously in groups of three, with two rats received the passive injection of cocaine or saline, was employed. Later, we examined whether acute treatment with the classical antidepressant imipramine or GABA(B) receptor ligands could alter the increases in immobility recorded after discontinuation of self-administered cocaine. We found a significant increase (44%) in the immobility time 3 days following discontinuation of cocaine (0.5mg/kg/infusion/2h daily) self-administration for 14 days; such enhancement resembled that observed in rats following the chronic mild stress. Acute administration with imipramine (15 or 30 mg/kg), the GABA(B) receptor agonists baclofen (0.125 mg/kg) and SKF 97541 (0.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related GABA Receptor Products

CAS 77337-73-6 Acamprosate calcium

Acamprosate calcium
(CAS: 77337-73-6)

Acamprosate calcium is a gamma-aminobutyric acid(GABA)agonist and modulator of glutamatergic systems. It has been used in alcohol dependence treatments and may ...

(CAS: 1159600-41-5)

This active molecular is a highly selective inverse agonist/negative allosteric modulator GABAAα5 receptors. It was developed by Roche to treat cognitive impair...

CAS 339-72-0 L-Cycloserine

(CAS: 339-72-0)

L-Cycloserine is excitatory amino acid, an antibiotic effective against Mycobacterium tuberculosis.

CAS 56776-32-0 Etifoxine Hydrochloride

Etifoxine Hydrochloride
(CAS: 56776-32-0)

Etifoxine Hydrochloride is Potentiator of GABAA receptor with anxiolytic and anticonvulsant activity.

CGP 54626 hydrochloride
(CAS: 149184-21-4)

The hydrochloride salt form of CGP 54626, a dichloropheny derivative, has been found to be a GABAB receptor antagonist that could probably be effective as an an...

CAS 62666-20-0 Progabide

(CAS: 62666-20-0)

Progabide is a gamma-aminobutyric acid (GABA) antagonist. It has agonistic activity for both the GABAA and GABAB receptors. It has antiepileptic activity and is...

CAS 840486-93-3 adipiplon

(CAS: 840486-93-3)

Adipiplon is GABAA receptor partial agonist. It can bind to the α3 subtype. Adipiplon is one of the first drugs selected for clinical development which is able ...

CAS 21715-46-8 Etifoxine

(CAS: 21715-46-8)

Etifoxine, also called as HOE 36801 or Stresam, is a positive allosteric modulator of GABAreceptors that produces anxiolytic effects by preferentially modulatin...

CAS 15291-75-5 Ginkgolide A

Ginkgolide A
(CAS: 15291-75-5)

Ginkgolide A is an extract from in Ginkgo biloba and a g-aminobutyric acid (GABA) antagonist with a Ki of 14.5 μM.

(CAS: 733717-87-8)

CH-50911 is a selective GABA-B antagonist with IC50 value of 1.1 μM. It is developed by Schering-Plough Corporation. CH-50911 is often used in pharmacology rese...

(CAS: 344413-67-8)

Lesogaberan is a potent and selective GABAB receptor agonist that limit the clinical use of baclofen for the treatment of GERD.

CAS 138729-47-2 Eszopiclone

(CAS: 138729-47-2)

Eszopiclone is an active stereoisomer of zopiclone with hypnotic and sedative activity and without significant anxiolytic activity. Eszopiclone is a GABA A rece...

Pipequaline HCl

The hydrochloride of pipequaline. Pipequaline is a non-selective GABAA receptor partial agonist that is potentially used as an anxiolytic drug of the nonbenzodi...

Remimazolam benzenesulfonat
(CAS: 1001415-66-2)

Remimazolam, a novel Benzodiazepine derivatives, has potential use for anxiolytic, sedative and hypnotic. For the reason that remimazolam's beding discontinued ...

CAS 56287-74-2 Afloqualone

(CAS: 56287-74-2)

Afloqualone is a agonist of GABA receptor has sedative and muscle-relaxant effects.

MK 0343
(CAS: 233275-76-8)

MK 0343, also known as MRK-409, is a subtype-selective GABAA partial agonist (Ki values are 0.21, 0.22, 0.23 and 0.40 for α3, α1, α5 and α2 respectively). MK-03...

GS 39783
(CAS: 39069-52-8)

GS 39783 is an allosteric positive modulator of GABAB receptors, decreases cocaine self-administration, blocks the rewarding properties of nicotine and produces...

CAS 64-65-3 Bemegride

(CAS: 64-65-3)

Bemegride is a central nervous system stimulant and antidote for barbiturate poisoning.

CAS 951650-22-9 NS 11394

NS 11394
(CAS: 951650-22-9)

NS 11394 is a drug with selectivity for the α3 and α5 subtypes. It acts as a subtype-selective positive allosteric modulator at GABAA receptors. It is used as a...

CAS 207306-50-1 TB 21007

TB 21007
(CAS: 207306-50-1)

TB 21007, as a nootropic drug, is a GABAA receptor inverse agonist selective for the α5-subtype (Ki values are 1.6, 16, 20 and 20 nM for α5, α2, α1 and α3 subty...

Chemical Structure

CAS 57717-80-3 CGP7930

Quick Inquiry

Verification code

Featured Items