Cardiovascular effects of CPU-23, a novel L-type calcium channel blocker with a unique molecular structure

British Journal of Pharmacology
H DongC R Triggle

Abstract

1. The cardiovascular effects of CPU-23 (1-[1-[(6-methoxy)-naphth-2-yl]]-ethyl-2-(1-piperidinyl)-acetyl-6, 7-dimethoxy-1,2,3,4-tetrahydroisoquinoline), a cleavage product of tetrandrine, were investigated using the whole cell perforated patch-clamp technique, in vitro tension measurements and in vivo haemodynamic recordings. 2. CPU-23 (1 and 10 microM) dose-dependently reduced concentration-response curves for KCl and phenylephrine (PE) in the rat tail artery; inhibition of KCl-induced contraction was much more potent than for PE. At the same concentrations, CPU-23 inhibited the inward Ba2+ currents in single smooth muscle cells isolated from the rat tail artery, while CPU-23 (10 microM) produced 95% vasorelaxation of the rat middle cerebral artery preconstricted with BayK 8644. 3. CPU-23 (10 and 30 microM) inhibited the noradrenaline-induced phasic contraction of the rat tail artery in the absence of extracellular Ca2+ from 40% of control to 23% and 14%, respectively (P<0.01) and tonic contraction of the artery after addition of Ca2+ (2 mM) from 100% of control to 83% and 75%, respectively (P<0.01). In the presence of extracellular Ca2+ the PE-induced contraction was reduced by CPU-23 (30 and 100 microM) to 27% and 37%, respec...Continue Reading

References

Jan 1, 1977·Annual Review of Pharmacology and Toxicology·A Fleckenstein
Apr 15, 1976·Nature·M J Mulvany, W Halpern
Sep 1, 1992·British Journal of Pharmacology·H DongS X Peng
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Jan 1, 1985·Cardiology·C R ContiJ A Hill
Sep 1, 1985·Circulation·P D Henry
Sep 1, 1994·Nihon yakurigaku zasshi. Folia pharmacologica Japonica·K Miyata, K Honda

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Citations

Dec 6, 2003·Canadian Journal of Anaesthesia = Journal Canadien D'anesthésie·Cécile BarelQuadiri Timour
Apr 29, 2000·Acta Anaesthesiologica Scandinavica·J Poelaert, C Roosens

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