Calcium channels in muscle cells isolated from rat mesenteric arteries: Modulation by dihydropyridine drugs

B. P. Bean, Michael Sturek, A. Puga, K. Hermsmeyer

Research output: Contribution to journalArticle

232 Citations (Scopus)

Abstract

The patch clamp technique was used to make whole-cell recordings of calcium channel currents from single muscle cells freshly isolated from rat mesenteric arteries. The cells were found to contain two types of calcium channels; one type is activated by small depolarizations and inactivates quickly, whereas the other requires stronger depolarizations for activation and inactivates more slowly. Nitrendipine blocked the second type of channels with a potency that depended on membrane potential. Interpreted by a modulated receptor hypothesis, these results suggest that nitrendipine binds to the inactivated state of the channel with a K(D) of about 0.5 nM, similar to concentrations effective in relaxing blood vessels. The magnitude of the calcium channel current was small compared with other excitable cells, but the 'calcium agonist' drug BAY K8644 produced a 10-fold augmentation of calcium channel current, suggesting the existence of a large 'reserve' of calcium channel current.

Original languageEnglish (US)
Pages (from-to)229-235
Number of pages7
JournalCirculation Research
Volume59
Issue number2
StatePublished - 1986
Externally publishedYes

Fingerprint

Mesenteric Arteries
Calcium Channels
Muscle Cells
Nitrendipine
Pharmaceutical Preparations
Patch-Clamp Techniques
Membrane Potentials
Blood Vessels
1,4-dihydropyridine
Calcium

ASJC Scopus subject areas

  • Physiology
  • Cardiology and Cardiovascular Medicine

Cite this

Calcium channels in muscle cells isolated from rat mesenteric arteries : Modulation by dihydropyridine drugs. / Bean, B. P.; Sturek, Michael; Puga, A.; Hermsmeyer, K.

In: Circulation Research, Vol. 59, No. 2, 1986, p. 229-235.

Research output: Contribution to journalArticle

@article{a5e22ad860cb4a6f89f604f34c1e078e,
title = "Calcium channels in muscle cells isolated from rat mesenteric arteries: Modulation by dihydropyridine drugs",
abstract = "The patch clamp technique was used to make whole-cell recordings of calcium channel currents from single muscle cells freshly isolated from rat mesenteric arteries. The cells were found to contain two types of calcium channels; one type is activated by small depolarizations and inactivates quickly, whereas the other requires stronger depolarizations for activation and inactivates more slowly. Nitrendipine blocked the second type of channels with a potency that depended on membrane potential. Interpreted by a modulated receptor hypothesis, these results suggest that nitrendipine binds to the inactivated state of the channel with a K(D) of about 0.5 nM, similar to concentrations effective in relaxing blood vessels. The magnitude of the calcium channel current was small compared with other excitable cells, but the 'calcium agonist' drug BAY K8644 produced a 10-fold augmentation of calcium channel current, suggesting the existence of a large 'reserve' of calcium channel current.",
author = "Bean, {B. P.} and Michael Sturek and A. Puga and K. Hermsmeyer",
year = "1986",
language = "English (US)",
volume = "59",
pages = "229--235",
journal = "Circulation Research",
issn = "0009-7330",
publisher = "Lippincott Williams and Wilkins",
number = "2",

}

TY - JOUR

T1 - Calcium channels in muscle cells isolated from rat mesenteric arteries

T2 - Modulation by dihydropyridine drugs

AU - Bean, B. P.

AU - Sturek, Michael

AU - Puga, A.

AU - Hermsmeyer, K.

PY - 1986

Y1 - 1986

N2 - The patch clamp technique was used to make whole-cell recordings of calcium channel currents from single muscle cells freshly isolated from rat mesenteric arteries. The cells were found to contain two types of calcium channels; one type is activated by small depolarizations and inactivates quickly, whereas the other requires stronger depolarizations for activation and inactivates more slowly. Nitrendipine blocked the second type of channels with a potency that depended on membrane potential. Interpreted by a modulated receptor hypothesis, these results suggest that nitrendipine binds to the inactivated state of the channel with a K(D) of about 0.5 nM, similar to concentrations effective in relaxing blood vessels. The magnitude of the calcium channel current was small compared with other excitable cells, but the 'calcium agonist' drug BAY K8644 produced a 10-fold augmentation of calcium channel current, suggesting the existence of a large 'reserve' of calcium channel current.

AB - The patch clamp technique was used to make whole-cell recordings of calcium channel currents from single muscle cells freshly isolated from rat mesenteric arteries. The cells were found to contain two types of calcium channels; one type is activated by small depolarizations and inactivates quickly, whereas the other requires stronger depolarizations for activation and inactivates more slowly. Nitrendipine blocked the second type of channels with a potency that depended on membrane potential. Interpreted by a modulated receptor hypothesis, these results suggest that nitrendipine binds to the inactivated state of the channel with a K(D) of about 0.5 nM, similar to concentrations effective in relaxing blood vessels. The magnitude of the calcium channel current was small compared with other excitable cells, but the 'calcium agonist' drug BAY K8644 produced a 10-fold augmentation of calcium channel current, suggesting the existence of a large 'reserve' of calcium channel current.

UR - http://www.scopus.com/inward/record.url?scp=0022551124&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0022551124&partnerID=8YFLogxK

M3 - Article

C2 - 2427250

AN - SCOPUS:0022551124

VL - 59

SP - 229

EP - 235

JO - Circulation Research

JF - Circulation Research

SN - 0009-7330

IS - 2

ER -