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Vasorelaxant and negative inotropic effects of gallopamil and LU49700, a metabolite of gallopamil, on isolated rat aorta and guinea-pig ventricular myocardium.

Authors
  • Noguchi, K
  • Takahashi, K
  • Kaneko, K
  • Higuchi, S
Type
Published Article
Journal
Arzneimittel-Forschung
Publication Date
Jan 01, 1998
Volume
48
Issue
1
Pages
22–25
Identifiers
PMID: 9522026
Source
Medline
License
Unknown

Abstract

The effects of LU49700 (CAS 116759-60-5), the main metabolite of gallopamil (CAS 16662-47-8) on the mechanical response of isolated rat aortic and guinea-pig ventricular papillary muscle preparations were compared with those of gallopamil. Gallopamil and LU49700 inhibited the 64 mmol/l KCl-induced contraction of rat aorta in a concentration-dependent manner. The vasorelaxant potency of LU49700 was 244 times weaker than that of gallopamil. Gallopamil and LU49700 produced concentration-dependent negative inotropic effects on isolated right ventricular papillary muscles. The negative inotropic potency of LU49700 was 418 times weaker than that of gallopamil. These findings indicate that LU49700 has a weaker cardiovascular depressant potency than gallopamil. Therefore, LU49700 may not mediate the effects of gallopamil for treating subjects with cardiovascular diseases.

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