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Vol. 295, Issue 2, 810-817, November 2000
1D-Adrenoceptors in Rat Aorta1
Departamento de Farmacología, Facultad de Farmacia,
Universitat de València, València, Spain
After depletion of intracellular calcium stores sensitive to
noradrenaline, a spontaneous increase in the resting tone (IRT) when
incubated in Ca2+-containing solution was observed in
isolated rat aorta, but not in tail artery. This IRT does not depend on
agonist activation of 
1-adrenoceptors but it is
inhibited by prazosin. A close relationship was found between the
inhibitory potencies of prazosin (pIC50 = 9.833), BMY
7378 (pIC50 = 8.924), and 5-methylurapidil
(pIC50 = 7.883) against IRT and their affinities for
cloned 1D-adrenoceptors. Chloroethylclonidine (100 µmol · l
1) did not inhibit the IRT. After
depletion of internal calcium stores by noradrenaline in absence of the
agonist, loading in Ca2+-containing solution also brings
about an increase in the inositol phosphate (IP) levels in rat aorta
(not seen in tail artery) that is inhibited by prazosin (1 µmol · l1), BMY 7378 (10 µmol · l1), and 5-methylurapidil (10 µmol · l1), thus confirming the results obtained in
contractile studies. Chloroethylclonidine (100 µmol · l1) did not inhibit this IP accumulation.
The fact that the IRT and the IP accumulation related to it can be
selectively inhibited by different 1-adrenoceptor
antagonists suggests the existence of a population of
1D-adrenoceptors that show constitutive activity in rat
aorta, not in tail artery.
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