当前位置： SCI文献检索 > EUROPEAN JOURNAL OF PHARMACOLOGY期刊下所有文献 > Electropharmacological effects of UK-1745, a novel cardiotonic drug, in guinea-pig ventricular myocytes.

Electropharmacological effects of UK-1745, a novel cardiotonic drug, in guinea-pig ventricular myocytes.

Abstract：

:Effects of (2RS, 3SR)-2-aminomethyl-2,3,7,8-tetrahydro-2,3,5,8, 8-pentamethyl-6H-furo-[2,3-e] indol-7-one hydrochloride (UK-1745), a novel cardiotonic drug with beta-adrenoceptor blocking property and antiarrhythmic activity, on the action potentials of isolated papillary muscles and the membrane currents of single ventricular myocytes of guinea pigs were examined and compared with those of milrinone using conventional microelectrode and patch-clamp techniques. In papillary muscles, UK-1745 (3-100 microM) produced a mild positive inotropic response and depressed the maximum upstroke velocity of the action potential (V(max)) at 100 microM. Milrinone, a phosphodiesterase III inhibitor, markedly shortened the action potential duration with a significant increase in developed tension. In enzymatically-dissociated ventricular myocytes, UK-1745 failed to increase the L-type Ca(2+) current (I(Ca)) at 10 and 30 microM and rather decreased I(Ca) at 100 microM. The high concentration of UK-1745 slightly inhibited the delayed rectifier K(+) current (I(K)). Although UK-1745 antagonized the isoproterenol-induced increase in I(Ca), it potentiated the histamine-induced increase in I(Ca). On the other hand, milrinone per se significantly increased I(Ca) and markedly enhanced the isoproterenol-induced increase in I(Ca). It can be concluded that UK-1745 is a unique cardiotonic drug possessing beta-adrenoceptor blocking and weak phosphodiesterase-inhibitory actions in addition to direct inhibitory actions on the Na(+), Ca(2+) and K(+) channels with its high concentrations.

journal_name

Eur J Pharmacol

journal_title

European journal of pharmacology

authors

Uemura H,Sakamoto N,Nakaya H

doi

10.1016/s0014-2999(99)00651-2

keywords:

subject

Has Abstract

pub_date

1999-11-03 00:00:00

pages

361-71

issue

3

eissn

0014-2999

issn

1879-0712

pii

S0014-2999(99)00651-2

journal_volume

383

pub_type

杂志文章

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