In 1990 we reported a randomized controlled trial in which the administration of regular inhaled β2-agonist therapy was associated with a deterioration in asthma control in a majority of subjects when compared to as-required β-agonist treatment [1]. There were more asthma exacerbations, reductions in the forced expiratory volume in one second (FEV1) and morning peak expiratory flow rates (PEFRs...

BACKGROUND Alterations in brain density and signaling associated with monoamine receptors are believed to play a role in depressive disorders. This study evaluates the functional status of α₂(A)-adrenoceptors in postmortem frontal cortex of depressed subjects. METHODS G-protein activation and inhibition of adenylyl cyclase (AC) activity induced by the α₂-adrenoceptor agonist UK14304 were meas...

The effects of selective manipulations of activity of the serotonergic and noradrenergic systems were examined in the rat model of visceral pain. It was found that neither p-chlorophenylalanine(p-CPA)- nor N-chloro-ethyl-2,2--bromo-benzylamine(DSP-4)-induced strong and selective depletion of the brain and spinal cord serotonin and noradrenaline, respectively, changed in a significant way rat vi...

BACKGROUND Experimental studies on the effects of alpha 2-adrenoceptors on regional coronary blood flow in normal and ischemic myocardium are highly controversial. A beneficial effect on regional ischemic myocardium has been demonstrated in different animal preparations with either alpha 2-adrenoceptor blockade or stimulation. Animal studies also demonstrated that postsynaptic alpha 2-adrenocep...

Percutaneous inoculation with herpes simplex virus type-1 brings about herpes zoster-like skin lesions, tactile allodynia, and mechanical hyperalgesia in mice. This study was conducted to determine whether the sympathetic nervous system and alpha-adrenoceptors would be involved in these pain-related responses and whether the alpha(2)-adrenoceptor agonist clonidine would suppress these responses...

Here, we describe the preclinical pharmacological profile of 5-[(R)-2-(5,6-diethyl-indan-2-ylamino)-1-hydroxy-ethyl]-8hydroxy-1H-quinolin-2-one (indacaterol), a novel, chirally pure inhaled 2 adrenoceptor agonist, in comparison with marketed drugs. Indacaterol is close to a full agonist at the human 2 adrenoceptor (Emax 73 1% of the maximal effect of isoprenaline; pEC50 8.06 0.02), whereas salm...

Beitzel, Felice, Paul Gregorevic, James G. Ryall, David R. Plant, Martin N. Sillence, and Gordon S. Lynch. 2-Adrenoceptor agonist fenoterol enhances functional repair of regenerating rat skeletal muscle after injury. J Appl Physiol 96: 1385–1392, 2004. First published November 7, 2003; 10.1152/japplphysiol.01081.2003.— 2-Adrenoceptor agonists such as fenoterol are anabolic in skeletal muscle, a...