I. Sayet et al., RAT VENA-CAVA ALPHA(1B)-ADRENOCEPTORS - CHARACTERIZATION BY [H-3] PRAZOSIN BINDING AND CONTRACTION EXPERIMENTS, European journal of pharmacology. Molecular pharmacology section, 246(3), 1993, pp. 275-281
We examined which subtypes of alpha1-adrenoceptors are expressed in ra
t vena cava by using both functional and [H-3]prazosin binding experim
ents. Pretreatment with chloroethylclonidine inactivated about 80% of
the speCifiC [H-3]prazosin binding sites and reduced the maximal norad
renaline-induced contraction to the same extent. Competition with subt
ype-selective agonists and antagonists showed primarily the alpha1B-ad
renoceptor subtype in vena cava. The number of al-adrenoceptors estima
ted with [H-3]prazosin binding and the maximal noradrenaline-induced c
ontraction were dose-dependently inhibited by phenoxybenzamine, indica
ting the absence of receptor reserve for noradrenaline in vena cava. A
s the noradrenaline-induced contraction was largely inhibited in Ca2+-
free solution, these results suggest that alpha1B-adrenoceptors can be
mainly linked to Ca2+ influx in rat vena cava.