Progabide

Progabide is a gamma-aminobutyric acid receptor (GABA) agonist.

Signaling Pathways >> Others >> Others

Research Areas >> Neurological Disease

GABA receptor[1]

Progabide is a gamma-aminobutyric acid receptor (GABA) agonist. Doses of 50, 100 and 200 mg/kg Progabide given IP to male Wistar rats increase the plasma corticosterone levels by 244, 365 and 476% respectively (t=6.44 to12.55, p<0.01). 10 mg/kg of Progabide fails to change the concentration of corticosterone in plasma (t=0.76, N.S.). The increased plasma corticosterone level induced by administration of 200 mg/kg Progabide is evident 30 (t=2.625, p<0.05), 60 (t=13.13, p<0.001) and 120 min (t=4.07, p<0.01) after drug injection, but returns to the control value 240 min after drug injection (t=0.86, N.S.). The greatest corticosterone rise (compare with the corresponding control) is reached 60 min following the administration of Progabide[1].

Male Wistar rats weighing 170 to 240 g are caged in groups of three under diurnal lighting conditions with free access to food and water. The rats are accustomed to handling (housing 1 per cage for 30 min, injecting with saline, 1 mL/100 g body weight) in the period of 7 days before the beginning of the experiment. Progabide is injected as a suspension in saline containing 0.1% Tween 80. Control rats are treated IP with the corresponding vehicle (1 mL/100 g body weight). Ether stress is performed and 15 min after the beginning of the stressful procedure the animals are sacrificed[1].

[1]. Manev H, et al. Progabide, a GABA mimetic drug, stimulates the secretion of plasma corticosterone in rats. Pharmacol Biochem Behav. 1987 Dec;28(4):443-6.

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MOLECULAR FORMULA :

C17-H16-Cl-F-N2-O2

MOLECULAR WEIGHT :

334.80

WISWESSER LINE NOTATION :

ZV3NUYR DG&R BQ EF

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

1350 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

LMSED6 L.E.R.S. Monograph Series. Laboratories d'Etudes et de Recherches Synthelabo Monograph Series. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) V.1- 1983- Volume(issue)/page/year: 3,203,1985

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

1350 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

LMSED6 L.E.R.S. Monograph Series. Laboratories d'Etudes et de Recherches Synthelabo Monograph Series. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) V.1- 1983- Volume(issue)/page/year: 3,203,1985

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intraperitoneal

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

900 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #4094992 ** TUMORIGENIC DATA **

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

655 gm/kg/2Y-C

TOXIC EFFECTS :

Tumorigenic - neoplastic by RTECS criteria Endocrine - adrenal cortex tumors

REFERENCE :

LMSED6 L.E.R.S. Monograph Series. Laboratories d'Etudes et de Recherches Synthelabo Monograph Series. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) V.1- 1983- Volume(issue)/page/year: 3,203,1985