CGP7930 - CAS 57717-80-3
Catalog number:
57717-80-3
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C19H32O2
Molecular Weight:
292.46
COA:
Inquire
Targets:
GABA Receptor
Description:
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.
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Purity:
>98 %
Appearance:
White solid
Synonyms:
3,5-Bis(1,1-dimethylethyl)-4-hydroxy-beta,beta-dimethylbenzenepropanol;2,6-Ditert-butyl-4-(3-hydroxy-2,2-dimethylpropyl)phenol;3-(3',5'-Di-tert-butyl-4'-hydroxy)phenyl-2,2-dimethylpropanol;CGP-7930
Solubility:
DMSO: 22 mg/mL, soluble
Storage:
2-8ºC
MSDS:
Inquire
Application:
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
Quantity:
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)
Density:
0.971±0.06 g/cm3 | Condition: Temp: 20 °C Press: 760 Torr
InChIKey:
XLWJPQQFJNGUPA-UHFFFAOYSA-N
InChI:
InChI=1S/C19H32O2/c1-17(2,3)14-9-13(11-19(7,8)12-20)10-15(16(14)21)18(4,5)6/h9-10,20-21H,11-12H2,1-8H3
Canonical SMILES:
CC(C)(C)C1=CC(=CC(=C1O)C(C)(C)C)CC(C)(C)CO
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.
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CAS 57717-80-3 CGP7930

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