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May 1, 1982Journal of Cardiovascular Pharmacology

Verapamil Competitively Inhibits α1-Adrenergic and Muscarinic but Not β-Adrenergic Receptors in Rat Myocardium

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Why the study?

Does verapamil inhibit alpha 1-adrenergic, muscarinic, and beta-adrenergic receptors in rat myocardium?

Population

Membranes prepared from rat heart (atria and ventricles)

Comparison

Verapamil and its derivative D-600 vs Baseline binding without verapamil

Design

Preclinical

Authors

JKJoel S. KarlinerSchreiner UniversityHMHarvey MotulskyFondazione GraphiTechJDJanet DunlapUniversity of California, San Diego

Discussion

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Implication

Does not support practice change; leaves open mechanistic relevance to human cardiac effects.

Structured PICO

Does verapamil inhibit alpha 1-adrenergic, muscarinic, and beta-adrenergic receptors in rat myocardium?

P
Population
Membranes prepared from rat heart (atria and ventricles)
I
Intervention
Verapamil (at concentrations including 10 microM, 30 microM, and 100 microM) and its derivative D-600
C
Comparator
Baseline binding without verapamil
O
Outcome
Binding affinity (Ki, KD) and maximal binding capacity (Bmax) of [3H]prazosin (alpha 1-adrenergic), [3H]QNB (muscarinic), and [3H]DHA (beta-adrenergic)surrogate

Verapamil competitively inhibits alpha 1-adrenergic and muscarinic receptors at clinically relevant concentrations in rat myocardium, suggesting these mechanisms may contribute to its cardiac effects.

Cite This Study

Karliner et al. (1982) studied this question.

synapsesocial.com/papers/6a843f7fde69cb059c72f9dbhttps://doi.org/10.1097/00005344-198205000-00025
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Also Consider

Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context:

  1. 1Relationship between the stereoselective negative inotropic effects of verapamil enantiomers and their binding to putative calcium channels in human heart1985 · 48 citations
  2. 2[3H]‐verapamil binding to rat cardiac sarcolemmal membrane fragments; an effect of ischaemia1987 · 19 citations
  3. 3Interaction of the Calcium Channel Activating3H-Bay K 8644 and Inhibiting3H-Verapamil with Specific Receptor Sites on Cultured Beating Myocardial Cells1984 · 14 citations
  4. 4Calcium Channel Inhibitor, Verapamil, Inhibits the Voltage-Dependent K+ Channels in Rabbit Coronary Smooth Muscle Cells2010 · 24 citations
  5. 5Effects of verapamil on (Na+ + K+)-ATPase, Ca2+-ATPase, and adenylate cyclase activity in a membrane fraction from rat and guinea pig ventricular muscle1977 · 6 citations