1 In rat isolated vas deferens, the isotonic contractile responses to low doses of noradrenaline or adrenaline were antagonized, and those to high doses were potentiated, by yohimbine, piperoxan, phentolamine and tolazoline. Effects due to intermediate doses were not affected, or were potentiated within about 30 min, following an initial inhibition. 2 The alpha-adrenoceptor blockers thus caused...

From the molecular mechanism of antagonist unbinding in the β(1) and β(2) adrenoceptors investigated by steered molecular dynamics, we attempt to provide further possibilities of ligand subtype and subspecies selectivity. We have simulated unbinding of β(1)-selective Esmolol and β(2)-selective ICI-118551 from both receptors to the extracellular environment and found distinct molecular features ...

The extended duration of bronchodilation due to formoterol and salmeterol greatly exceeds that of short acting beta 2-adrenoceptor agonists, such as salbutamol or terbutaline. This extended duration and their capacity to "reassert" airway smooth muscle relaxation in vitro despite repeated washing has prompted considerable debate on the underlying mechanism(s). The comparative pharmacology, and ...

Karim, F., and S. M. Poucher. b-Adrenoceptors in vascular capacitance responses to unloading of carotid baroreceptors in anesthetized dogs. Am. J. Physiol. 273 (Heart Circ. Physiol. 42): H1713–H1718, 1997.—The role of band aadrenoceptors in the total vascular capacitance responses to changing pressure in vascularly isolated carotid sinuses of anesthetized and atropinized dogs was investigated. ...

Earlier studies suggest that alpha2-adrenoceptor antagonists and dopamine receptor agonists may enhance sexual activity in human and nonhuman male primates. It is not known whether these compounds influence the sexual behavior of female primates. We determined whether the administration of a selective alpha2-adrenoceptor antagonist (atipamezole), a dopamine receptor agonist (apomorphine), or th...

BACKGROUND The purpose of this study was to evaluate the gender-related changes in the function and distribution of α(1)-adrenoceptors in the distal mesenteric artery of streptozotocin (STZ)-induced diabetic rats at the level of α(1)-adrenoceptor subtypes. METHODS Diabetes was induced by intravenous injection of STZ in a dose of 60 mg/kg through the tail vein in 8 week-old male or female Spra...

The existence of atypical- or beta 3-adrenoceptors has now been generally accepted. These receptors have been shown to be abundant in adipose tissue and in a number of gastrointestinal smooth muscle preparations. A recent study reported that beta 3-adrenoceptor stimulation mediated relaxation of isolated canine bronchial smooth muscle. The aim of the present study was to extend this observation...

This review evaluates the role of α-adrenoceptor antagonists as a potential treatment of prostate cancer (PCa). Cochrane, Google Scholar and Pubmed were accessed to retrieve sixty-two articles for analysis. In vitro studies demonstrate that doxazosin, prazosin and terazosin (quinazoline α-antagonists) induce apoptosis, decrease cell growth, and proliferation in PC-3, LNCaP and DU-145 cell lines...

Using topical instillation of non-selective and selective beta-adrenoceptor antagonists we examine the proposal that a deficit in inhibitory sympathetic innervation of ciliary smooth muscle may be a specific precursor to the onset and development of late-onset myopia (LOM). Post-task accommodative hysteresis, a possible consequence of such a deficit, was assessed by measuring the time-course of...

BACKGROUND AND PURPOSE Tryptamine increases blood pressure by vasoconstriction, but little is known about its actions on the mesentery, in particular the resistance arteries. Tryptamine interacts with trace amine-associated receptors (TAARs) and because of its structural similarity to 5-HT, it may also interact with 5-HT receptors. Our hypothesis is therefore that the rat mesenteric arterial be...