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September 1, 1990British Journal of Pharmacology21 citationsOpen Access

Evidence that agonist and antagonist enantiomers of the dihydropyridine PN 202–791 act at different sites on the voltage‐dependent calcium channel of vascular muscle

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AHAlun D. HughesSHSteffen HeringTBT. B. Bolton

Structured PICO

Do agonist and antagonist enantiomers of PN 202-791 act at different sites on voltage-dependent calcium channels in rabbit vascular muscle cells?

P
Population
Isolated ear artery cells of the rabbit
I
Intervention
S(+)-PN 202-791 (calcium channel agonist) and R(-)-PN 202-791 (calcium channel antagonist)
C
Comparator
Presence of the other enantiomer
O
Outcome
Inward current carried by barium through voltage-dependent calcium channelssurrogate

The agonist and antagonist enantiomers of the dihydropyridine PN 202-791 appear to act at two separate binding sites on the voltage-dependent calcium channel of vascular muscle.

Abstract

S(+)-PN 202-791, a calcium channel agonist, and its optical isomer R(-)-PN 202-791, a calcium channel antagonist, respectively increased and decreased inward current carried by barium through voltage-dependent calcium channels in isolated ear artery cells of the rabbit in a concentration-dependent manner. The EC50 or IC50 derived from the concentration-response relationship was unaltered in the presence of the other enantiomer indicating that no competitive antagonism exists between these enantiomers and suggesting that the actions of these two enantiomers involve two separate binding sites.

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Cite This Study

Hughes et al. (1990) studied this question.

synapsesocial.com/papers/6a8388a513ebf8b47e9609e2https://doi.org/10.1111/j.1476-5381.1990.tb12076.x
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