The binding of [³H]‐diazepam to guinea‐pig ileal longitudinal muscle and the in vitro inhibition of contraction by benzodiazepines

Abstract

1The longitudinal muscle-myenteric plexus strip preparation of the guinea-pig ileum was used to study the binding of

Central and Peripheral Neurotoxic Effects of Ivermectin in Rats

“…However, diazepam does not affect the contractions induced by acetylcholine, 5-HT, histamine and electrical stimulation. Contrary to these results, Hullihan et al [17] found that diazepam produced a dose-dependent decrease in the electrically induced contractions of a longitudinal ileal muscle strip and antagonized the contractions induced by K + , Ca 2+ , histamine and carbachol. Another benzodiazepine, tetrazepam, produced concentration-dependent and complete relaxation of muscle contractions induced by KCl (80 mM) in the guinea pig ileum, and this relaxant action was not antagonized by pretreatment with hexamethonium (0.1 mM), an antagonist for nicotinic receptors, atropine (1 M), an antagonist for muscarinic receptors, or PK 11195 (1 M) antagonist for peripheral-type benzodiazepine receptors [34].…”

Interaction of calcium channel blockers with non-neuronal benzodiazepine binding sites.

“…The physiological significance of the non-neuronal benzodiazepine binding site is as yet unknown despite the presence of a high density of such sites in a wide variety of tissues (5)(6)(7)(8)(9)(10)(11)(12)(13)(14)(15). Recently, however, several pharmacological effects have been ascribed to agents acting at these sites, and a common mechanism of action, that of calcium antagonism, has been suggested by these findings.…”

“…Benzodiazepines also bind to membranes from a variety of other tissues including kidney (5,6), heart (6, 7), lung (5,6), liver (5,6), mast cells (6), platelets (8), intestinal smooth muscle (9), several cell lines (10,11), and central nervous system non-neuronal elements (12)(13)(14)(15). The sites on these latter cell types represent a population of binding sites pharmacologically distinct from the neuronal type because of the different structural requirements for their respective ligands (unpublished data).…”

“…Furthermore, the non-neuronal site is not modified by y-aminobutyric acid and does not bind other neuronal-type ligands such as the f3-carbolines (14). Although a specific function has not yet been ascribed to the non-neuronal sites, recent evidence suggests that agents acting at these sites may interfere with calcium-dependent activities in vitro (9,11,16).…”

Diazepam ve baklofenin kobaylarda sidik kesesi düz kası üzerine etkileri

“…Ayrıca yabani memelilerin hareketsiz bırakılarak yakalanmaları ile bunların sağaltım ve zoolojik işlemlerini kolaylaştır-mada, hareketsiz kılıcı madde olarak yararlanılmaktadır (1,3,4,9). Bundan başka insanlarda geniş ölçekli kas gevşetici, antikonvülzan, anksiyolitik ve hipnotik amaç-larla uygulandığı da bilinmektedir (7,8,19).…”