| Autor: |
Hullihan JP, Spector S, Taniguchi T, Wang JK |
| Jazyk: |
angličtina |
| Zdroj: |
British journal of pharmacology [Br J Pharmacol] 1983 Feb; Vol. 78 (2), pp. 321-7. |
| DOI: |
10.1111/j.1476-5381.1983.tb09397.x |
| Abstrakt: |
1--The longitudinal muscle-myenteric plexus strip preparation of the guinea-pig ileum was used to study the binding of [3H]-diazepam and the effect of benzodiazepines on its contraction. 2--Scatchard analysis of binding indicated a single class of binding sites with KD = 43 nM and Bmax = 229 fmol/mg prótein. Binding was of peripheral type based on the much greater binding affinity of Ro5-4864 as compared to clonazepam. Binding of [3H]-diazepam reached equilibrium at 10 min and dissociated rapidly (T1/2 = 1.3 min). The KD derived from the rate constants agreed with that from the Scatchard analysis. 3--Benzodiazepines produced a dose-dependent decrease in the electrically induced contractions of the longitudinal muscle strip, but their potencies in this effect did not correlate with their binding affinities. 4--Diazepam antagonized the contractions of the longitudinal muscle strip induced by K+, Ca2+, histamine and carbachol. The inhibition of Ca2+-induced contractions was reversed by increasing the concentration of Ca2+ in the medium. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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