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  • 1
    Electronic Resource
    Electronic Resource
    Oxford, UK : Blackwell Science Ltd
    Autonomic & autacoid pharmacology 25 (2005), S. 0 
    ISSN: 1474-8673
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Chemistry and Pharmacology , Medicine
    Notes: 1 The pressor action of noradrenaline and its blockade by selective α1-adrenoceptor antagonists in the pithed mouse were evaluated. 2 Chloroethylclonidine (α1B/D-adrenoceptor alkylating agent) or BMY 7378 (α1D-adrenoceptor antagonist), both at 1 mg kg−1, did not block the increase in blood pressure induced by noradrenaline. 3 5-Methylurapidil (α1A-adrenoceptor antagonist), at 0.1 mg kg−1, displaced the dose–response curve approximately six-fold to the right. 4 The results support the idea that the pithed mouse vasculature express α1A-adrenoceptors and suggest that it is a good model to study the roles of α1-adrenoceptors in gene knockout or overexpression.
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Oxford, UK : Blackwell Science Ltd
    Autonomic & autacoid pharmacology 25 (2005), S. 0 
    ISSN: 1474-8673
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Chemistry and Pharmacology , Medicine
    Notes: 1 The effect of WAY 405 ((R)-N-(2-methyl-(4-indolyl-1-piperazinyl)ethyl)-N-(2-pyridinyl) cyclohexane carboxamide), a putative 5-HT1A receptor antagonist, on cardiovascular function was studied. 2 In anaesthetized rats, the i.v. injection of WAY 405 did not significantly modify basal heart rate nor blood pressure at doses of 1, 3, 10 and 30 μg kg−1; while the antagonist dose dependently antagonized the 5-HT1A receptor agonist, 8-OH-DPAT (8-hydroxy-2-(di-n-propylamino)tetralin)-induced hypotension and bradycardia. 3 WAY 405 antagonized noradrenaline-induced contraction in isolated arteries, with pKB values of 6.6 ± 0.1, 6.5 ± 0.1 and 6.5 ± 0.1, for rat tail artery (α1A-adrenoceptors), rabbit aorta (α1B-adrenoceptors), and rat aorta (α1D-adrenoceptors) respectively. 4 The results show that in the control of blood pressure the new compound, WAY 405, behaves as a silent 5-HT1A receptor antagonist in the anaesthetized rat, also having low affinity for vascular α1-adrenoceptors.
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  • 3
    ISSN: 1474-8673
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Chemistry and Pharmacology , Medicine
    Notes: 1 The effect of WAY100635 (N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-(2-pyridinyl) cyclohexanecarboxamide trihydrochloride), a 5-HT1A receptor antagonist, on cardiovascular function was studied. 2 The i.v. injection of WAY100635 dose-dependently decreased blood pressure in anaesthetized rats; while in pithed rats WAY100635 (1 mg  kg−1) displaced the phenylephrine pressor effect. 3 WAY100635 antagonized phenylephrine-induced contraction in rabbit and rat aorta (pA2 of 6.88 and 7.93 and Schild slopes of −0.83 and −1.21, respectively); while in rat caudal artery pKB was 7.45 and the Schild slope of −0.56, suggesting a complex interaction in this vessel. 4 The results show that WAY100635 induced hypotension in the anaesthetized rat and suggest that this effect could be partially explained by antagonism of vascular α1-adrenoceptors.
    Type of Medium: Electronic Resource
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