BACKGROUND Current therapy for relieving bronchoconstriction may be ineffective in severe asthma, particularly in the small airways. The aim of this study was to further characterise responses to the recently identified novel bronchodilators rosiglitazone (RGZ) and chloroquine (CQ) under conditions where β-adrenoceptor agonist efficacy was limited or impaired in mouse small airways within lung ...

The importance of cell phenotype in determining the molecular mechanisms underlying β2-adrenoceptor (β2AR) function has been noted previously when comparing responses primary cells and recombinant model lines. Here, we have generated haplotype-specific SNAP-tagged β2AR human embryonic stem (ES) lines applied fluorescence correlation spectroscopy (FCS) to study surface receptors progenitor diffe...

Kawai, Hiroya, Amy Mohan, Jason Hagen, Erdan Dong, Jacqueline Armstrong, Suzanne Y. Stevens, and Chang-seng Liang. Alterations in cardiac adrenergic terminal function and b-adrenoceptor density in pacing-induced heart failure. Am J Physiol Heart Circ Physiol 278: H1708– H1716, 2000.—Congestive heart failure is associated with cardiac adrenergic nerve terminal changes and b-adrenoceptor density ...

Antibodies against cholinergic and adrenergic receptors (adrenoceptors) are frequent in serum of patients with chronic heart failure. Their prevalence is associated with Chagas' disease, idiopathic dilated cardiomyopathy (DCM), and ischaemic heart disease. Among the epitopes targeted are first and second extracellular loops of the β-adrenergic (β-adrenoceptor) and M2 muscarinic receptor. β(1)-a...

The present study was designed to measure norepinephrine release during sympathetic nerve stimulation and evaluate the presynaptic inhibitory and facilitatory actions of a-adrenoceptor and /3-adrenoceptor agonists respectively, in the isolated perfused kidney of normotensive WistarKyoto (WKY) and spontaneously hypertensive rats (SHR). Periarterial nerve stimulation (0.25 to 32 Hz) caused a sign...

BACKGROUND Contrary to beta(1)- and beta(2)-adrenoceptors, beta(3)-adrenoceptors mediate a negative inotropic effect in human ventricular muscle. To assess their functional role in heart failure, our purpose was to compare the expression and contractile effect of beta(3)-adrenoceptors in nonfailing and failing human hearts. METHODS AND RESULTS We analyzed left ventricular samples from 29 fail...

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 ...

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...

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...

Although nitrous oxide (N(2)O) has been used to facilitate surgery for >150 years, its molecular mechanism of action is not yet defined. Having established that N(2)O-induced release of norepinephrine mediates the analgesic action at alpha(2) adrenoceptors in the spinal cord, we now investigated whether activation of noradrenergic nuclei in the brainstem is responsible for this analgesic action...