beta-Adrenergic agonists are potent relaxing agents of airway smooth muscle; however, they are often incapable of fully reversing agonist-mediated contractions. The present study was designed to quantitate the relationship between beta-adrenoceptor binding, signal transduction, and relaxation in rabbit tracheal smooth muscle (TSM). TSM segments contracted with acetylcholine to 25 to 75% maximal...

Do β3-adrenoceptor agonists cause urinary bladder smooth muscle relaxation by inhibiting 1 acetylcholine release? 2 Focus on “Inhibition of cholinergic neurotransmission by β3-adrenoceptors depends on 3 adenosine release and A1 receptors activation in human and rat urinary bladder” 4 5 Katerina Okeke, Stavros Gravas, Martin C. Michel 6 7 8 Dept. of Pharmacology, Johannes Gutenberg University, M...

The present study explored the hypothesis that a prolonged 8 weeks exposure to a high fructose intake suppresses adrenergic and angiotensin II (Ang II)-mediated vasoconstriction and is associated with a higher contribution of α1D-adrenoceptors. A total of thirty-two Sprague-Dawley rats received either 20 % fructose solution (FFR) or tap water (control, C) to drink ad libitum for 8 weeks. Metabo...

This study was performed to characterize the -adrenoceptor population in rabbit isolated corpus cavernosum (RbCC) by using nonselective and selective -adrenoceptor agonists and antagonists in functional assays. Metaproterenol, ritodrine, fenoterol, and 8-hydroxy-5-[(1R)-1-hydroxy-2-[N-[(1R)-2-( -methoxyphenyl)-1-methylethyl]amino]ethyl]carbostyril (TA 2005) (3–100 nmol each) dose dependently re...

The search for drugs with anorectic activity, acting within the adrenergic system has attracted the interest of researchers. Partial α2-adrenoceptor agonists might offer the potential for effective and safe treatment of obesity. We compared the effectiveness and safety of α2-adrenoceptor ligands in reducing body mass. We also analyzed if antagonist and partial agonists of α2-adrenoceptor--yohim...

In the last decades new pharmacodynamic properties of beta-adrenoceptors have been discovered that could greatly impact in the use of beta-adrenergic agents in the clinical practice. Concepts such as multiple binding sites, constitutive activity, polymorphism and intracellular signaling of betaadrenoceptors may contribute in the discovery of more efficacious pharmacological agents for treatment...

Some large vessels have a mixed functional population of postjunctional α1- and α 2-adrenoceptors. The purpose of the work presented here was to investigate the population of postjunctional α -adrenoceptors in the rat isolated common carotid artelY Male Wi star rats were killed by overdose with pentobarbitone sodium, after which the left and right common carotid arteries were removed. Rings...

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....

Pyridostigmine bromide (PB) is a reversible cholinesterase inhibitor used routinely in the treatment of myasthenia gravis and recently by the US Army as a prophylactic agent against potential nerve gas attack in the Persian Gulf War. Pyridostigmine has been implicated as one of several possible causative factors associated with Persian Gulf illnesses. To investigate toxic interactions between P...

Pharmacological characteristics of the canine isolated splenic artery were investigated by the cannula insertion method for observing vascular responses to vasoactive agents and periarterial nerve stimulation. Four alpha-adrenoceptor agonists and tyramine induced vasoconstrictions in a dose-dependent manner, and the order of potency was noradrenaline (NA) > phenylephrine > clonidine > methoxami...