Diazepam is not a direct allosteric modulator of α1‐adrenoceptors, but modulates receptor signaling by inhibiting phosphodiesterase‐4

Diazepam is not a direct allosteric modulator of α1‐adrenoceptors, but modulates receptor signaling by inhibiting phosphodiesterase‐4

Abstract α1A‐ and α1B‐adrenoceptors (ARs) are G protein‐coupled receptors (GPCRs) that are activated by adrenaline and noradrenaline to modulate smooth muscle contraction in the periphery, and neuronal outputs in the central nervous system (CNS). α1A‐ and α1B‐AR are clinically targeted with antagoni...

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Bibliographic Details
Main Authors: Lisa M. Williams, Xiaoji He, Tasneem M. Vaid, Alaa Abdul‐Ridha, Alice R. Whitehead, Paul R. Gooley, Ross A.D. Bathgate, Spencer J. Williams, Daniel J. Scott
Format: Article
Language:English
Published: Wiley 2019-02-01
Series:Pharmacology Research & Perspectives
Subjects:
α1 adrenergic receptors
α1‐adrenoceptors
allosteric modulator
benzodiazepines
GPR68
phosphodiesterase
Online Access:https://doi.org/10.1002/prp2.455

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