ChemInform Abstract: SYNTHESIS AND HYPOTENSIVE ACTIVITY OF N‐ALKYL‐N′′‐CYANO‐N′‐PYRIDYLGUANIDINES

Petersen, H; Nielsen, C. K.; Arrigoni-Martelli, E

doi:10.1002/chin.197852224

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“…Pinacidil is a vasodilator currently under clinical investigation as a potential anti-hypertensive agent (Petersen et al, 1978;Arrigoni-Martelli et al, 1980;Carlsen et al, 1981;Bray et al, 1987;Cook et al, 1988). The main mechanism by which this drug relaxes vascular smooth muscle tissues is thought to be activation of a K channel which may be Ca-dependent (Bray et al, 1987;Cook et al, 1988;Hermsmeyer, 1988;Videbaek et al, 1988).…”

Section: Introductionmentioning

confidence: 99%

Pinacidil inhibits neuromuscular transmission indirectly in the guinea‐pig and rabbit mesenteric arteries

Nakashima

Seki

et al. 1990

British J Pharmacology

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1 Effects of pinacidil were investigated on neuromuscular transmission in smooth muscle tissues of the rabbit and guinea-pig mesenteric arteries by both electrophysiological procedures and a bioassay of noradrenaline (NA) outflows. 2 Pinacidil (over 1 aM) hyperpolarized smooth muscle cell membranes in both tissues, in a concentration dependent manner. Pinacidil hyperpolarized and increased the ionic conductance of smooth muscle membrane more markedly in the rabbit mesenteric artery than in the guinea-pig. The hyperpolarization induced by pinacidil occurred in the presence or absence of endothelial cells and was blocked by glibenclamide. 3 Perivascular adrenergic nerve stimulation produced excitatory junction potentials (ej.ps) and repetitive stimulation produced a facilitation of ej.ps in both tissues. Pinacidil (over 1 piM) reduced the amplitude and the decay time of ej.ps to a consistently greater extent in the rabbit mesenteric artery than in the guinea-pig. However, the facilitation process of ej.ps was not modified following application of pinacidil (1 pM). The pinacidil-induced inhibition of ej.ps was prevented by pretreatment with glibenclamide.4 Pinacidil (30pM) marginally increased the overflows of NA and its metabolite, 3,4-dihydroxyphenylglycol (DOPEG) released following repetitive perivascular nerve stimulations. 5 Pinacidil (10pM) partly inhibited the voltage-dependent Ca channel, as estimated from the recovery process following removal of pinacidil, of action potentials evoked on ej.ps. 6 It is concluded that pinacidil increases ionic conductance and hyperpolarizes smooth muscle cell membranes of the guinea-pig and rabbit mesenteric arteries and as a consequence, inhibits the neuromuscular transmission process occurring on adrenergic nerve stimulation with no reduction in the amount of released transmitter.

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Section: Introductionmentioning

confidence: 99%

Pinacidil inhibits neuromuscular transmission indirectly in the guinea‐pig and rabbit mesenteric arteries

Nakashima

Seki

et al. 1990

British J Pharmacology

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ChemInform Abstract: SYNTHESIS AND HYPOTENSIVE ACTIVITY OF N‐ALKYL‐N′′‐CYANO‐N′‐PYRIDYLGUANIDINES

Abstract: Aus den Thioharnstoffen (I) entstehen die Carbodiimide (II), die mit Cyanamid (III) in die Addukte (IV) übergeführt werden.

Cited by 1 publication

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Pinacidil inhibits neuromuscular transmission indirectly in the guinea‐pig and rabbit mesenteric arteries

Pinacidil inhibits neuromuscular transmission indirectly in the guinea‐pig and rabbit mesenteric arteries

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