Circulation, Vol 84, 1-14, Copyright © 1991 by American Heart Association
V Ralevic and G Burnstock
Characterization of P2-purinoceptor subtypes has facilitated understanding
of the many diverse effects produced by purine nucleotides.
P2X-Purinoceptors are located on vascular smooth muscle where they mediate
vasoconstriction resulting from ATP released as a cotransmitter with
noradrenaline from sympathetic nerves. P2Y- Purinoceptors are usually
located on the vascular endothelium where they have a role as mediators of
vascular relaxation by locally produced ATP. In some vessels,
P2Y-purinoceptors are also located on the smooth muscle, perhaps in
association with purinergic or sensory nerves, where they can elicit direct
relaxation to neuronally released ATP. The net effect of ATP and its
analogues on isolated vessels or on vascular beds will be the results of
actions mediated by P2X- and P2Y- purinoceptor subtypes, although changes
in vascular tone and in integrity of nerves and endothelial cells may alter
the balance of the response. Such changes have been observed in diseased
states (e.g., atherosclerosis) and may have important implications for the
involvement of P2-purinoceptors in, for example, vasospasm. The development
of selective and potent antagonists to P2X- and P2Y- purinoceptors has so
far remained elusive, and their therapeutic potential can only be guessed.
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Roles of P2-purinoceptors in the cardiovascular system [published erratum appears in Circulation 1991 Nov;84(5):2212]
University College, London, UK.
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