Subtypes of functional α1-adrenoceptor |
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Authors: | James R Docherty |
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Institution: | (1) Department of Physiology, Royal College of Surgeons in Ireland, 123, St. Stephen’s Green, Dublin 2, Ireland |
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Abstract: | In this review, subtypes of functional α1-adrenoceptor are discussed. These are cell membrane receptors, belonging to the
seven-transmembrane-spanning G-protein-linked family of receptors, which respond to the physiological agonist noradrenaline.
α1-Adrenoceptors can be divided into α1A-, α1B- and α1D-adrenoceptors, all of which mediate contractile responses involving
Gq/11 and inositol phosphate turnover. A fourth α1-adrenoceptor, the α1L-, represents a functional phenotype of the α1A-adrenoceptor.
α1-Adrenoceptor subtype knock-out mice have refined our knowledge of the functions of α-adrenoceptor subtypes, particuarly
as subtype-selective agonists and antagonists are not available for all subtypes. α1-Adrenoceptors function as stimulatory
receptors involved particularly in smooth muscle contraction, especially contraction of vascular smooth muscle, both in local
vasoconstriction and in the control of blood pressure and temperature, and contraction of the prostate and bladder neck. Central
actions are now being elucidated. |
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