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Pivagabine

Names

[ CAS No. ]:
69542-93-4

[ Name ]:
Pivagabine

[Synonym ]:
4-(2,2-dimethylpropanoylamino)butanoic acid

Biological Activity

[Description]:

Pivagabine (CXB 722), a psychoactive drug, is a hydrophobic 4-aminobutyric acid derivative with neuromodulatory activity. Pivagabine penetrates the blood-brain barrier in rats. Pivagabine antagonizes the effects of foot shock on both GABAA receptor function and corticotropin-releasing factor (CRF) concentrations in rat brain[1][2].

[Related Catalog]:

Signaling Pathways >> Others >> Others
Research Areas >> Neurological Disease

[In Vivo]

Pivagabine (CXB 722) (200 mg/kg; i.p.; twice a day for 4 days and 1 hour before killing on the 5th day) prevents the effects of foot-shock stress on CRF concentration in both brain regions[2]. Animal Model: Adult male Sprague-Dawley CD rats (200-250 g)[2] Dosage: 200 mg/kg Administration: i.p.; twice a day for 4 days and 1 hour before killing on the 5th day Result: Prevented the effects of foot-shock stress on CRF concentration in both brain regions. Reduced by 52% the CRF concentration in the hypothalamus but had no effect on that in the cerebral cortex.

[References]

[1]. Esposito G, et al. Pivagabine: a novel psychoactive drug. Arzneimittelforschung. 1997 Nov;47(11A):1306-9.

[2]. Serra M, et al. Antagonism by pivagabine of stress-induced changes in GABAA receptor function and corticotropin-releasing factor concentrations in rat brain. Psychoneuroendocrinology. 1999 Apr;24(3):269-84.

Chemical & Physical Properties

[ Density]:
1.053g/cm3

[ Boiling Point ]:
397ºC at 760 mmHg

[ Molecular Formula ]:
C9H17NO3

[ Molecular Weight ]:
187.23600

[ Flash Point ]:
193.9ºC

[ Exact Mass ]:
187.12100

[ PSA ]:
69.89000

[ LogP ]:
1.85380

[ Index of Refraction ]:
1.462

[ Storage condition ]:
2-8°C