Detail of "84379-13-5"

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The benzodiazepine partial receptor agonist, bretazenil, provokes a strong hyperphagic response: A meal pattern analysis in free feeding rats

The benzodiazepine partial receptor agonist, bretazenil, provokes a strong hyperphagic response: A meal pattern analysis in free feeding rats. Clifton, P. G.; Cooper, S. J. (Laboratory Experimental Psychology, University Sussex, Brighton BN1 9QG, UK). Behavioural Pharmacology, 7(5), 454-461 (English) 1996 Rapid Science Publishers. CODEN: BPHAEL. ISSN: 0955-8810. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) In this report we characterize the effects of the benzodiazepine receptor partial agonist bretazenil (0.Several reagents with their cas registry numbers 84379-13-5 and 12794-10-4 are used here.1-3 mg/kg) on meal patterning and satiety sequences of male rats. Expt. 1 indicated that bretazenil (0.3-1.0 mg/kg) doubled the size of the first meal; there was no concurrent increase in feeding rate and effects on water intake were smaller. Expt. 2 showed that the benzodiazepine receptor antagonist ZK93426 (10 mg/kg) blocked this effect on meal size; in addn. ZK93426 reduced water intake in the first 2 h following drug administration, which we attribute to its weak inverse agonist action. Expt. 3 examd. satiety sequences after bretazenil treatment. Food intake and feeding behavior were enhanced; in the following behavioral sequence, active and grooming behavior patterns were reduced and resting was greatly increased. The data are discussed in relation to current theories of benzodiazepine action on food intake and the processing of taste stimuli. .

Blockade of behavioral effects of bretazenil by flumazenil and ZK 93,426 in pigeons

Blockade of behavioral effects of bretazenil by flumazenil and ZK 93,426 in pigeons. Witkin, J. M.; Acri, J. B.; Gleeson, S.; Barrett, J. E. (Drug Development Group, Preclinical Pharmacology, Addiction Research Center, National Institute on Drug Abuse, National Institutes of Health, Baltimore, MD 21224, USA).Some commonly used reagents like 84379-13-5 is used in this experiment. Pharmacology, Biochemistry and Behavior, 56(1), 1-7 (English) 1997 Elsevier. CODEN: PBBHAU. ISSN: 0091-3057. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Benzodiazepine receptor partial agonists manifest full efficacy in preclin. tests of anxiolytic drug action but do not fully reproduce the discriminative stimulus effects of benzodiazepine receptor full agonists in pigeons. The partial agonist, bretazenil, binds to both diazepam-sensitive and diazepam-insensitive GABAA receptors. Previous studies have suggested a role for each of these receptor populations in some behavioral effects of bretazenil in pigeons. A possible role for these receptor subtypes in the behavioral effects of bretazenil was further investigated through drug interaction studies with the benzodiazepine receptor antagonists, flumazenil and ZK 93,426. Whereas flumazenil binds with high affinity to both receptor isoforms, ZK 93,426 binds preferentially to diazepam-sensitive binding sites. Bretazenil markedly increased punished responding of pigeons without significantly affecting nonpunished responding. In pigeons discriminating the full benzodiazepine receptor agonist, midazolam, from saline, bretazenil produced only 60-75% maximal effect. Flumazenil and ZK 93,426 neither increased punished responding nor substituted for midazolam, but dose-dependently blocked the effects of bretazenil on punished responding. Flumazenil also dose-dependently blocked the effects of bretazenil in midazolam-discriminating pigeons, whereas ZK 93,426 only attenuated this effect. These results indicate that bretazenil's actions as a partial agonist at diazepam-sensitive benzodiazepine receptors mediate increases in punished responding and substitution for the discriminative stimulus effects of midazolam in pigeons. The differences in the effects of flumazenil and ZK 93,426 on the discriminative stimulus effects of bretazenil suggest a potential contribution of diazepam-insensitive sites to this behavioral effect. .