Intraperitoneal (IP) injection of bupropion (3,6, amine (4,16 mg kg•') induced dose-dependent climbing in mice. The climbing response induced by both drugs were decreased in animals pretreated either with the 0-1 antagonist SCH 233<)0 or the 0-2 antagonist sulpiride. The α-adrenoceptor blocker phenoxybenzamine decreased the climbing induced by both bupropion and amphetamine, but the β-ad...

(R)-6-[(3-{[4-(5-{[2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethyl]amino}pent-1-yn-1-yl)phenyl] carbamoyl}phenyl)sulphonyl]-4-[(3-methoxyphenyl)amino]-8-methylquinoline-3-carboxamide trifluoroacetic acid (GS-5759) is a bifunctional ligand composed of a quinolinone-containing pharmacophore [β2-adrenoceptor agonist orthostere (β2A)] found in several β2-adrenoceptor agonists, including...

Cholinergic and adrenergic tones were calculated for three different teleost fish species: Gadus morhua, Labrus bergylta, and Sparus aurata using atropine as a muscarinic receptor antagonist and either sotalol or propranolol as β-adrenoceptor antagonists. Depending on the order of administration of atropine and the two β-adrenoceptor antagonists, it was observed that propranolol but not sotalol...

During hyperthermia, vasoconstrictor tone in the viscera is lost despite high levels of sympathetic neural outflow and plasma catecholamines, suggesting that vascular responsiveness to adrenergic receptor stimulation is reduced. The purpose of this study was to determine whether adrenoceptor-mediated control of vascular resistance is altered at high body core temperatures. The hemodynamic respo...

β-Adrenoceptor antagonists differ in their degree of partial agonism. In vitro assays have provided information on ligand affinity, selectivity, and intrinsic efficacy. However, the extent to which these properties are manifest in vivo is less clear. Conscious freely moving rats, instrumented for measurement of heart rate (β1; HR) and hindquarters vascular conductance (β2; HVC) were used to mea...

The spontaneously hypertensive rat (SHR) has been proposed as an overactive bladder model, driven, at least partially, by alterations in bladder innervation. To assess the functional role of sensory bladder afferents we evaluated the conscious cystometric response to prostaglandin E(2) (PGE(2)) or acetic acid (AA) bladder infusion. SHR demonstrated a hypersensitivity to PGE(2) and AA, as indica...