Potentiation of the effects of γ-amino-butyric acid and adenosine on the vas deferens by diazepam and clobazam

✍ Scribed by P. Slater; M. W. R. Bennett

• Publisher: John Wiley and Sons
• Year: 1982
• Tongue: English
• Weight: 382 KB
• Volume: 2
• Category: Article
• ISSN: 0272-4391
• DOI: 10.1002/ddr.430010714

✦ Synopsis

Potentiation of the effects of y-aminobutyric acid and adenosine on the vas deferens by diazepam and clobazam. Drug Dev. Res. S1:095-100, 1982.

The aim of the study was to investigate the effects of the 1,4-benzodiazepine diazepam and the 1,5-benzodiazepine clobazam on the inhibition of the isotonically recorded, electrically induced twitch contractions of the guinea pig and rat vas deferens preparations induced y-aminobutyric acid (GAB) (GABA, receptors) and adenosine (purine receptors).

Both benzodiazepines (10-6 -10-5 M) potentiated GABA, but clobazam was more potent. In contrast, diazepam (104 -3 x 10-5 M) was more potent than clobazam in potentiating adenosine. Several other 1,4-benzodiazepines were tested. These exhibited a wide range of potencies: the rank order for potentiating GABA differed from the potency order for potentiating adenosine. It is concluded that benzodiazepines, by an unknown mechanism, potentiate the effects of GABA, receptor stimulation. The mechanism is probably independent of the inhibition of adenosine uptake, which is responsible for potentiating purinereceptor activity.