Identification of calcium-channel receptors in intact animals.

William R Roeske, H. R. Lee, H. I. Yamamura, H. Schoemaker

Research output: Contribution to journalArticle

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Abstract

In this study, we demonstrate the in vivo labeling by [3H]nitrendipine ([3H]NTD) of peripheral tissues and the brain in Sprague-Dawley rats. Specific binding is decreased in a dose-dependent manner by nifedipine, with a mean inhibitory dose of 2-10 mg/kg (i.p.). Thin-layer chromatography of the particulate-bound radioactivity reveals that the predominant tritiated drug bound in the left ventricle and the cerebral cortex is [3H]NTD, whereas metabolites constitute the main species in the liver. Peak radioactivity is seen at 15 min following an intravenous injection of [3H]NTD. Highly perfused tissues such as the heart, brain, and lung have significant [3H]NTD binding. In contrast to previously reported in vitro studies, [3H]NTD binding is low in the aorta, skeletal muscle, and ileum. This in vivo animal model is suitable for pharmacokinetic and physiological studies of the calcium channel in intact animals.

Original languageEnglish (US)
Pages (from-to)71-82
Number of pages12
JournalAdvances in myocardiology
Volume6
StatePublished - 1985
Externally publishedYes

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Calcium-Sensing Receptors
Calcium Channels
Radioactivity
Nitrendipine
Brain
Nifedipine
Thin Layer Chromatography
Ileum
Intravenous Injections
Cerebral Cortex
Heart Ventricles
Sprague Dawley Rats
Aorta
Skeletal Muscle
Animal Models
Pharmacokinetics
Lung
Liver
Pharmaceutical Preparations
In Vitro Techniques

ASJC Scopus subject areas

  • Medicine(all)

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Roeske, W. R., Lee, H. R., Yamamura, H. I., & Schoemaker, H. (1985). Identification of calcium-channel receptors in intact animals. Advances in myocardiology, 6, 71-82.

Identification of calcium-channel receptors in intact animals. / Roeske, William R; Lee, H. R.; Yamamura, H. I.; Schoemaker, H.

In: Advances in myocardiology, Vol. 6, 1985, p. 71-82.

Research output: Contribution to journalArticle

Roeske, WR, Lee, HR, Yamamura, HI & Schoemaker, H 1985, 'Identification of calcium-channel receptors in intact animals.', Advances in myocardiology, vol. 6, pp. 71-82.
Roeske, William R ; Lee, H. R. ; Yamamura, H. I. ; Schoemaker, H. / Identification of calcium-channel receptors in intact animals. In: Advances in myocardiology. 1985 ; Vol. 6. pp. 71-82.
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