Abstract
The binding characteristics of the calcium-channel antagonist nitrendipine an analog of nifedipine, have been measured in plasma membrane enriched microsomal fractions from the canine thoracic aorta, canine mesenteric artery, and rat mesenteric artery. The dissociation constants, K(D) for the high-affinity binding sites were, respectively, 0.308, 0.254, and 0.101 nM and B(max) values for binding capacity were 20.3, 25.0, and 18.0 fmol/mg of microsomal protein. Studies with isolated tissues, in which the sensitivity of the high potassium mechanical response to nitrendipine was determined, indicate that the appearance K(D) for nitrendipine in the canine mesenteric artery, as reflected by the IC 50 (mean inhibition constant) value, is 4.5-5.3 nM and for the rat mesenteric artery 2.5-6.6 nM.
| Original language | English |
|---|---|
| Pages (from-to) | 1738-1741 |
| Number of pages | 4 |
| Journal | Canadian Journal of Physiology and Pharmacology |
| Volume | 60 |
| Issue number | 12 |
| State | Published - 1982 |
| Externally published | Yes |
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All Science Journal Classification (ASJC) codes
- Physiology
- Pharmacology
Cite this
Calcium-channel antagonist binding to isolated vascular smooth muscle membranes. / Triggle, C. R.; Agrawal, Devendra K.; Bolger, G. T.; Daniel, E. E.; Kwan, C. Y.; Luchowski, E. M.; Triggle, D. J.
In: Canadian Journal of Physiology and Pharmacology, Vol. 60, No. 12, 1982, p. 1738-1741.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Calcium-channel antagonist binding to isolated vascular smooth muscle membranes
AU - Triggle, C. R.
AU - Agrawal, Devendra K.
AU - Bolger, G. T.
AU - Daniel, E. E.
AU - Kwan, C. Y.
AU - Luchowski, E. M.
AU - Triggle, D. J.
PY - 1982
Y1 - 1982
N2 - The binding characteristics of the calcium-channel antagonist nitrendipine an analog of nifedipine, have been measured in plasma membrane enriched microsomal fractions from the canine thoracic aorta, canine mesenteric artery, and rat mesenteric artery. The dissociation constants, K(D) for the high-affinity binding sites were, respectively, 0.308, 0.254, and 0.101 nM and B(max) values for binding capacity were 20.3, 25.0, and 18.0 fmol/mg of microsomal protein. Studies with isolated tissues, in which the sensitivity of the high potassium mechanical response to nitrendipine was determined, indicate that the appearance K(D) for nitrendipine in the canine mesenteric artery, as reflected by the IC 50 (mean inhibition constant) value, is 4.5-5.3 nM and for the rat mesenteric artery 2.5-6.6 nM.
AB - The binding characteristics of the calcium-channel antagonist nitrendipine an analog of nifedipine, have been measured in plasma membrane enriched microsomal fractions from the canine thoracic aorta, canine mesenteric artery, and rat mesenteric artery. The dissociation constants, K(D) for the high-affinity binding sites were, respectively, 0.308, 0.254, and 0.101 nM and B(max) values for binding capacity were 20.3, 25.0, and 18.0 fmol/mg of microsomal protein. Studies with isolated tissues, in which the sensitivity of the high potassium mechanical response to nitrendipine was determined, indicate that the appearance K(D) for nitrendipine in the canine mesenteric artery, as reflected by the IC 50 (mean inhibition constant) value, is 4.5-5.3 nM and for the rat mesenteric artery 2.5-6.6 nM.
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M3 - Article
C2 - 7165866
AN - SCOPUS:0020413009
VL - 60
SP - 1738
EP - 1741
JO - Canadian Journal of Physiology and Pharmacology
JF - Canadian Journal of Physiology and Pharmacology
SN - 0008-4212
IS - 12
ER -