| Literature DB >> 1348445 |
G Costa1, M Isla, A García-Pascual, E Jimenez, P Recio, A Labadia, A García-Sacristán.
Abstract
1. In vitro experiments were designed to characterize postjunctional alpha-adrenoceptor subtypes in ring segments (1 mm length; outer diameter 300-500 microns) from arteries supplying the oviduct of the heifer. 2. Noradrenaline, adrenaline and phenylephrine evoked concentration-dependent contractile responses. The pD2 values were 5.67, 5.89 and 5.93, respectively. Medetomidine clonidine and B-HT 920 (2-amino-6-allyl-5,6,7,8-tetra-hydro-4H-(thiazo)-4,5-d-azepoine ) were ineffective. 3. The alpha-adrenoceptor selective antagonists, prazosin (1 nM-0.1 microM) and rauwolscine (0.1-10 microM) competitively antagonized the response to noradrenaline. The pA2 values were 9.38 and 6.83, respectively. 4. The dissociation constant (KD) for noradrenaline calculated by use of the irreversible antagonist, dibenamine, was 3.95 (2.09-5.81) microM. The occupancy-response relationship was non-linear. Half-maximal response to noradrenaline was obtained with 22% receptor occupancy while maximal response required 100% occupancy. 5. B-HT 920 evoked a biphasic contractile concentration-dependent response in preparations incubated in a physiological solution containing 20 mM K+, 0.1 microM prazosin and 1 microM propranolol. Rauwolscine 0.1 microM significantly (P less than 0.01) blocked the first component of the B-HT 920 concentration-response curve with an apparent pA2 value of 8.52 (7.86-9.18). 6. These results strongly suggest that alpha-adrenoceptors in oviductal arteries are mainly of the alpha 1 subtype, although a possible role for alpha 2-adrenoceptors cannot be excluded.Entities:
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Year: 1992 PMID: 1348445 PMCID: PMC1908651 DOI: 10.1111/j.1476-5381.1992.tb14262.x
Source DB: PubMed Journal: Br J Pharmacol ISSN: 0007-1188 Impact factor: 8.739