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pKI values of prazosin and idazoxan for receptors stimulated by neuronally released transmitter in the epididymal portion of rat isolated vas deferens.Journal List > Br J Pharmacol > v.111(1); Jan 1994SummarySelected ReferencesPage BrowsePDF (1.0M)ContentsArchiveRelated material:PubMed recordPubMed related artsPubMed LinkOutCompoundSubstancePubMed articles by: Mackay, D. Kengatharan, M.Br J Pharmacol. 1994 January; 111(1): 227–232. PMCID: PMC1910001Copyright notice pKI values of prazosin and idazoxan for receptors stimulated by neuronally released transmitter in the epididymal portion of rat isolated vas deferens.D. Mackay and M. KengatharanDepartment of Pharmacology, University of Leeds.Abstract1. A new method has been used to measure pKI values of prazosin and idazoxan against neuronally-released transmitter in the epididymal portion of the rat isolated vas deferens. The most reproducible results were obtained with a prolonged antagonist equilibration time (1 h). 2. Under these conditions the pKI of prazosin was practically unaffected by addition of alpha, beta-methylene-adenosine-5'-triphosphate (10 microM) to desensitize purinoceptors. Addition of desmethylimipramine (DMI) (0.3 microM) produced a small, but statistically non-significant, reduction. 3. The same method has been used to measure the pKI of prazosin against exogenous noradrenaline. In the latter case addition of DMI (0.3 microM) and corticosterone (30 microM) together produced a statistically significant reduction in the apparent pKI of prazosin. 4. The new method for estimating pKI values shows that DMI itself acts either pseudo-irreversibly or non-competitively and may be reducing the apparent pKI of prazosin. 5. The pKI values obtained for prazosin and idazoxan against neuronally-released transmitter are in good agreement with those obtained by other workers for the actions of these drugs on alpha-adrenoceptors.Full textFull text is available as a scanned copy of the original print version. Get a printable copy (PDF file) of the complete article (1.0M), or click on a page image below to browse page by page. Links to PubMed are also available for Selected References.227228229230В 231232Selected ReferencesThese references are in PubMed. This may not be the complete list of references from this article. Aboud R, Shafii M, Docherty JR. Investigation of the subtypes of alpha 1-adrenoceptor mediating contractions of rat aorta, vas deferens and spleen. Br J Pharmacol. 1993 May;109(1):80–87. [PubMed]Arunlakshana O, Schild HO. Some quantitative uses of drug antagonists. Br J Pharmacol Chemother. 1959 Mar;14(1):48–58. [PubMed]Brown DA, Docherty JR, French AM, MacDonald A, McGrath JC, Scott NC. Separation of adrenergic and non-adrenergic contractions to field stimulation in the rat vas deferens. Br J Pharmacol. 1983 Jun;79(2):379–393. [PubMed]Doxey JC, Roach AG, Smith CF. Studies on RX 781094: a selective, potent and specific antagonist of alpha 2-adrenoceptors. Br J Pharmacol. 1983 Mar;78(3):489–505. [PubMed]Mackay D. A new method for estimating dissociation constants of competitive and non-competitive antagonists with no prior knowledge of agonist concentrations. Br J Pharmacol. 1994 Jan;111(1):219–226. [PubMed]McCulloch MW, Story DF. Antagonism of noradrenaline and histamine by desipramine in the isolated artery of the rabbit ear. Br J Pharmacol. 1972 Sep;46(1):140–150. [PubMed]McGrath JC. Adrenergic and 'non-adrenergic' components in the contractile response of the vas deferens to a single indirect stimulus. J Physiol. 1978 Oct;283:23–39. [PubMed]Minneman KP, Fox AW, Abel PW. Occupancy of alpha 1-adrenergic receptors and contraction of rat vas deferens. Mol Pharmacol. 1983 Mar;23(2):359–368. [PubMed]Sneddon P, Burnstock G. Inhibition of excitatory junction potentials in guinea-pig vas deferens by alpha, beta-methylene-ATP: further evidence for ATP and noradrenaline as cotransmitters. Eur J Pharmacol. 1984 Apr 13;100(1):85–90. [PubMed]Stjärne L, Astrand P. Relative pre- and postjunctional roles of noradrenaline and adenosine 5'-triphosphate as neurotransmitters of the sympathetic nerves of guinea-pig and mouse vas deferens. Neuroscience. 1985 Mar;14(3):929–946. [PubMed]U'Prichard DC, Greenberg DA, Sheehan PP, Snyder SH. Tricyclic antidepressants: therapeutic properties and affinity for alpha-noradrenergic receptor binding sites in the brain. Science. 1978 Jan 13;199(4325):197–198. [PubMed]Ventura S, Pennefather JN. Sympathetic co-transmission to the cauda epididymis of the rat: characterization of postjunctional adrenoceptors and purinoceptors. Br J Pharmacol. 1991 Feb;102(2):540–544. 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