ChemInform Abstract: Synthesis and Antisecretory and Antiulcer Activities of Derivatives and Analogues of 2‐(2‐Pyridyl)tetrahydrothiophene‐2‐carbothioamide.

Aloup, Jean-Claude; Bouchaudon, J.; Farge, D.; James, C. J.; Deregnaucourt, J.; Hardy-Houis, Monique

doi:10.1002/chin.198723174

Cited by 1 publication

(1 citation statement)

References 1 publication

Supporting

Mentioning

Contrasting

Order By: Relevance

“…One of the most interesting new mol ecules is that derived from a series of K+/H+ exchange inhibitors [9] and typified by RP-49356 [10]. Little has so far been published about this agent, but there are no obvious indications of a really selective action.…”

Section: Introductionmentioning

confidence: 99%

The Potassium Channel Openers: A New Class of Vasorelaxants

Weston

Longmore²,

Newgreen³

et al. 1990

J Vasc Res

View full text Add to dashboard Cite

Cromakalim, pinacidil, nicorandil, diazoxide and RP- 49356 belong to the class of drugs termed potassium channel openers. In rat portal vein diazoxide, like cromakalim, abolished spontaneous mechanical and electrical activity and in rat aorta caused an increase in ⁸⁶Rb efflux and inhibited KCl (20 mM)-induced contractions. However, in contrast to cromakalim, diazoxide (>100 µM) also inhibited mechanical responses evoked by 80 mM KCl in rat aorta suggesting that it possesses pharmacological properties in addition to K channel opening. Since glibenclamide can attenuate the effects of cromakalim and diazoxide in vascular tissues, it is possible that a channel resembling the ATP-sensitive K channel found in pancreatic β-cells may be involved in the vasorelaxant effects of these agents. However, differences exist in the order of potency of cromakalim and diazoxide for producing smooth muscle relaxation and for decreasing insulin secretion in pancreatic β-cells. Furthermore galanin (which opens ATP-sensitive K channels in β-cells) increases mechanical activity in rat portal vein. It is anticipated that new chemical developments will produce K channel opening molecules with greater potency and tissue selectivity.

show abstract

Section: Introductionmentioning

confidence: 99%