BACKGROUND The aim of this study was to evaluate the effect of diabetes on the function and distribution of vascular α(1)-adrenoceptors in the abdominal aorta and distal mesenteric artery from streptozotocin (STZ)-induced diabetic rats at the level of the α(1)-adrenoceptor subtypes. METHODS Diabetes was induced by a single intravenous injection of STZ (60 mg/kg) in 8 week-old male Sprague-Daw...

Previous research has indicated that allosteric interactions across the dimer interface of β1-adrenoceptors may be responsible for a secondary low affinity binding conformation. Here we have investigated the potential for probe dependence, in the determination of antagonist pKi values at the human β1-adenoceptor, which may result from such allosterism interactions. Three fluorescent β1-adrenoce...

Background-Failure ofthe donor (graft) heart is the main cause ofmortality in the first month after orthotopic cardiac transplantation. In a preliminary study marked downregulation of cardiac fp adrenoceptor density was found in apparently normal donor hearts ofrecipients who developed severe cardiac failure soon after implantation. Cardiac fl adrenoceptors are an important factor in the develo...

BACKGROUND Meperidine proved to be more effective in treatment of shivering than equianalgesic doses of other opioids, especially pure mu-agonists. Further, meperidine has well known nonopioid actions including agonistic effects at alpha2-adrenoceptors in vitro. Accordingly, the authors investigated nonopioid receptor-mediated effects of meperidine on thermoregulation using a mice model of nons...

Dynamic exercise evokes sustained blood pressure and heart rate (HR) increases. Although it is well accepted that there is a CNS mediation of cardiovascular adjustments during dynamic exercise, information on the role of specific CNS structures is still limited. The bed nucleus of the stria terminalis (BST) is involved in exercise-evoked cardiovascular responses in rats. However, the specific n...

Neurokinin A (NKA) induces bronchoconstriction mediated by tachykinin NK(2) receptors in animals and humans, and may be increased in asthma. Because beta(2)-adrenoceptor agonists are the most widely used bronchodilators in asthma, we investigated the effects of the beta(2)-adrenoceptor agonist fenoterol on NK(2) receptor messenger RNA (mRNA) and receptor density as well as the functional respon...

We previously reported that nicotine-induced nitric oxide (NO)-mediated cerebral neurogenic vasodilation was dependent on intact sympathetic innervation. We hypothesized that nicotine acted on sympathetic nerve terminals to release norepinephrine (NE), which then acted on adrenoceptors located on the neighboring nitric oxidergic (NOergic) nerve terminals to release NO, resulting in vasodilation...

Although beta-adrenoceptor antagonists were first developed for their potential therapeutic uses in cardiac disease, it was soon recognized during clinical trials that they had effects on the central nervous system, some ofthem unwanted, but others ofpossible therapeutic value. This paper reviews some recent developments in this area of beta-adrenoceptor clinical pharmacology, earlier studies h...

Targeted disruption of mouse beta3-adrenoceptor was generated by homologous recombination, and validated by an acute in vivo study showing a complete lack of effect of the beta3-adrenoceptor agonist CL 316,243 on the metabolic rate of homozygous null (-/-) mice. In brown adipose tissue, beta3-adrenoceptor disruption induced a 66% decrease (P < 0.005) in beta1-adrenoceptor mRNA level, whereas le...

UNLABELLED α1-Adrenoceptor expression on nociceptors may play an important role in sympathetic-sensory coupling in certain neuropathic pain syndromes. The aim of this study was to determine whether α1-adrenoceptor expression was upregulated on surviving peptidergic, nonpeptidergic, and myelinated nerve fiber populations in the skin after chronic constriction injury of the sciatic nerve in rats....