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1 adrenoceptor subtypes in arteries: evidence of 1L as a functional isoform of the 1A adrenoceptor
1 Farmacologia, Facultad de Ciencias Experimentales y de la Salud. Universidad Cardenal Herrera-CEU., Moncada, Valencia, Spain; Instituto de Biomedicina de Valencia, CSIC, Valencia, Valencia, Spain
2 Farmacologia, Facultad de Farmacia. Universitat de Valencia., Burjassot, Valencia, Spain
3 Farmacologia, Facultad de Ciencias Experimentales y de la Salud. Universidad Cardenal Herrera-CEU., Moncada, Valencia, Spain
4 Instituto de Biomedicina de Valencia, CSIC, Valencia, Valencia, Spain
5 Farmacologia, Facultad de Farmacia. Universitat de Valencia., Burjassot, Valencia, Spain; Unidad Mixta CNIC-UVEG, Valencia, Valencia, Spain
* To whom correspondence should be addressed. E-mail: doconp{at}uv.es.
The mRNA levels for the three a1-adrenoceptor subtypes, 
1A, 1B and 1D were quantified by real-time RT-PCR in arteries from Wistar rats. The 1D-adrenoceptor was prominent in both aorta (79.0%) and mesenteric arteries (72.6%), 1A predominated in tail (61.7%) and small mesenteric artery (SMA: 73.3%), and both 1A and 1D subtypes were expressed at similar levels in iliac artery. The mRNA levels of the 1B subtype were a minority in all vessels (1.7-11.1 %). Concentration-response curves of contraction to phenylephrine or relaxation to 1-adrenoceptor antagonists on maximal sustained contraction induced by phenylephrine were constructed in vessels control or pretreated with 100 µmolL-1 chloroethylclonidine (CEC) for 30 min. The significant decrease in the phenylephrine potency observed after CEC treatment, together to the inhibitory potency displayed by BMY 7378 (1D adrenoceptor antagonist) confirm the relevant role of 1D adrenoceptors in aorta, iliac and proximal mesenteric artery. The potency of 5-methylurapidil (1A-adrenoceptor antagonist) and the changes in the potency of both BMY 7378 and 5 methylurapidil after CEC treatment provided evidence of a mixed population of 1A and 1D-adrenoceptors in iliac and distal mesenteric artery. The low potency of prazosin (pIC50 < 9) as well as the high 5-methylurapidil potency in the tail and SMA suggest the main role of 1A/1L-adrenoceptors with a minor participation of the 1D subtype. mRNA levels and CEC treatment corroborated this pattern and confirmed that the 1L adrenoceptor could be a functional isoform of the 1A subtype.
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