Abstract |
The potencies of seven benzodiazepines (BDZs) were established by three tests: inhibition of [3H] flunitrazepam receptor binding, inhibition of [3H] adenosine uptake, and prevention of pentylenetetrazol-induced seizures in mice. There is a high correlation between the potency for inhibition of [3H] flunitrazepam receptor binding and the antipentylenetetrazol potencies of benzodiazepines (r = 0.941; p less than 0.01). The antipentylenetetrazol potencies of benzodiazepines correlate well with their ability to inhibit [3H] adenosine uptake (r = 0.860; p less than 0.05 and greater than 0.01). However, there is no significant correlation between the potency for the inhibition of [3H] flunitrazepam receptor binding and the potency for inhibition of [3H] adenosine uptake (r = 0.751; p greater than 0.05). In addition, there is a marked difference in BDZ potency as measured by these two tests in vitro. The ratios of the Ki values (Ki2/Ki1) range from 98 for BDZ I to 64615 for clonazepam. The data presented indicate that antipentylenetetrazol activity of benzodiazepines results from an interaction between BDZ and nanomolar affinity BDZ receptors.
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Authors | A Y Chweh, E A Swinyard, H H Wolf |
Journal | Canadian journal of physiology and pharmacology
(Can J Physiol Pharmacol)
Vol. 62
Issue 1
Pg. 132-5
(Jan 1984)
ISSN: 0008-4212 [Print] Canada |
PMID | 6324977
(Publication Type: Journal Article, Research Support, U.S. Gov't, P.H.S.)
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Chemical References |
- Receptors, Cell Surface
- Receptors, GABA-A
- Tritium
- Benzodiazepines
- Flunitrazepam
- Adenosine
- Pentylenetetrazole
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Topics |
- Adenosine
(metabolism)
- Animals
- Benzodiazepines
(pharmacology)
- Flunitrazepam
(metabolism)
- Male
- Mice
- Pentylenetetrazole
(antagonists & inhibitors)
- Receptors, Cell Surface
(drug effects, metabolism)
- Receptors, GABA-A
- Seizures
(prevention & control)
- Tritium
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