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To examine the contribution of the sympathetic nervous system to the development of hypertension, we injected spontaneously hypertensive rat (SHR) pups and normotensive Wistar-Kyoto rat (WKY) pups twice daily with saline (1.0 mL/kg SC) or terazosin (0.5 mg/kg SC), an alpha 1-adrenoceptor antagonist, from postnatal day 1 through 21. We determined the effectiveness and duration of action of this terazosin dose in pilot studies with adult SHR and WKY. Body weights of WKY pups were greater than body weights of SHR pups from postnatal day 1 through 21. In addition, body weights of terazosin-treated pups of both strains were comparable to body weights of saline-injected littermate controls. Indirectly measured systolic pressures of terazosin-treated SHR were reduced significantly at 60 and 90 days of age but not at 30 days of age compared with saline-injected littermate controls. Terazosin did not affect systolic pressures of WKY, measured at 30, 60, and 90 days of age. At 100 days of age, in chronically catheterized rats, mean arterial pressures of terazosin-treated SHR were reduced significantly compared with those of saline-injected littermate controls. In contrast, terazosin did not affect mean arterial pressures of WKY at 100 days of age. Finally, preweanling treatment with terazosin did not alter patterns of open field behavior of adult SHR or WKY. SHR were significantly more active and reared more frequently compared with WKY. These findings indicate that the time between birth and weaning at 21 days of age is critical for the full expression of the hypertensive phenotype in SHR. Chronic blockage of alpha 1-adrenoceptors during the preweanling period in SHR may reduce vascular hypertrophy, leading to long-term reductions in arterial pressure.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=8621205&dopt=Abstract
J Pharmacol Exp Ther. 1996 Jun;277(3):1237-46.
Functional antagonistic activity of Rec 15/2739, a novel alpha-1 antagonist selective for the lower urinary tract, on noradrenaline-induced contraction of human prostate and mesenteric artery.
Testa R, Guarneri L, Taddei C, Poggesi E, Angelico P, Sartani A, Leonardi A, Gofrit ON, Meretyk S, Caine M.
Pharmaceutical R&D Division, Recordati S.p.A., Milano, Italy.
The aim of this study was to compare with known reference standards the functional in vitro alpha-1 antagonistic activity of Rec 15/2739 on noradrenaline-induced contractions of human prostate and mesenteric artery. We also characterized these tissues with regard to the alpha-1 adrenoceptor subtypes present. Comparing the apparent pKB values revealed Rec 15/2739 to be one of the most potent compounds action on the prostate. Its potency was slightly lower than that of tamsulosin and was higher than the potencies of prazosin, terazosin and 5-methylurapidil. On the mesenteric artery, tamsulosin was the most potent compound. Comparing the results from the functional studies with those obtained from radioreceptor binding studies, we found that the potency (pKB value) in inhibiting the contraction of prostatic tissue showed a close and significant correlation with the affinity for native and recombinant alpha-1A adrenoceptors. No significant correlation was found with affinity for either the native or the recombinant alpha-1B adrenoceptor subtype, or for recombinant alpha-1d receptors. Similar results were obtained for mesenteric artery. In order to characterize further the alpha-1 adrenoceptor subtypes present in the examined tissues, we investigated the functional effects of chloroethylclonidine, an alpha-1B-D subtypes selective alpha-1 adrenoceptor irreversible antagonist, and those of nifedipine, which antagonizes the extracellular calcium influx primarily mediated by alpha-1A adrenoceptor stimulation. The results indicate the presence of both chloroethylclonidine-sensitive and -insensitive alpha-1 adrenoceptor subtypes in the human prostate, whereas in mesenteric artery the alpha-1A subtype seems to be present exclusively. The possibility that the functionally relevant alpha-1 adrenoceptor subtype could be classified as alpha-1L in both tissues shoul also be considered.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=8667184&dopt=Abstract
J Recept Signal Transduct Res. 1995 Sep-Dec;15(7-8):863-85.
Actions of terazosin and its enantiomers at subtypes of alpha 1- and alpha 2-adrenoceptors in vitro.
Hancock AA, Buckner SA, Ireland LM, Knepper SM, Kerwin JF Jr.
Division of Neuroscience Research, Abbott Laboratories, Abbott Park, IL 60064-3500, USA.
Terazosin and its enantiomers, antagonists of alpha 1-adrenoceptors, were studied in radioligand binding and functional assays to determine relative potencies at subtypes of alpha 1- and alpha 2-adrenoceptors in vitro. The racemic compound and its enantiomers showed high and apparently equal affinity for subtypes of alpha 1-adrenoceptors with Kl values in the low nanomolar range, and showed potent antagonism of alpha 1-adrenoceptors in isolated tissues, with the enantiomers approximately equipotent to the racemate at each alpha 1-adrenoceptor subtype. At alpha 2b sites, R(+) terazosin bound less potently than either the S(-) enantiomer or racemate. R(+) terazosin was also less potent than the S(-) enantiomer or the racemate at rat atrial alpha 2B receptors. These agents were not significantly different in their potencies at alpha 2a or alpha 2A sites. Since the high affinity for alpha 2B sites of quinazoline-type alpha-adrenoceptor antagonists has been used to differentiate alpha 2-adrenoceptor subtypes, the low affinity of R(+) terazosin for these sites was unexpected. Because terazosin or its enantiomers are approximately equipotent at alpha 1-adrenoceptor subtypes, the lower potency of R(+) terazosin at alpha 2B receptors indicates a somewhat greater selectivity for alpha 1-compared to alpha 2B adrenoceptor subtypes. The possible pharmacological significance of this observation is discussed.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=8673721&dopt=Abstract
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