The nomenclature of the Adrenoceptors has been agreed by NC-IUPHAR Subcommittee on [64, 194]. Adrenoceptors, α1 three α1-adrenoceptor subtypes α1A, α1B and α1D are activated endogenous agonists (-)-adrenaline (-)-noradrenaline. -(-)phenylephrine, methoxamine cirazoline prazosin doxazosin antagonists considered selective for α1- relative to α2-adrenoceptors. [3H]prazosin [125I]HEAT (BE2254) rela...

the effect of epinephrine on phosphatidate phosphohydrolase (pap) activity of isolated human hepatocytes was studied. epineprine inhibited the enzyme activity progressively at concentrations above 0.1 µm, reaching a maximum inhibition of 64.5% at 100 µm concentration. inclusion of alprenolol, a β-receptor blocker, in the incubation mixture abolished the inhibitory effect of epinephrine on pap, ...

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...

Alpha1-adrenoceptors were identified in murine tissues by [3H]prazosin saturation binding studies, with a rank order of cerebral cortex > cerebellum > liver > lung > kidney > heart > spleen, with the spleen not exhibiting detectable expression. Competition binding studies were performed with 5-methylurapidil, BMY 7378, methoxamine, (+)-niguldipine, noradrenaline, SB 216469 and tamsulosin. On th...

BACKGROUND There are three turkey β-adrenoceptors: the original turkey β-adrenoceptor from erythrocytes (tβtrunc, for which the X-ray crystal structure has recently been determined), tβ3C and tβ4C-receptors. This study examined the similarities and differences between these avian receptors and mammalian receptors with regards to binding characteristics and functional high and low affinity agoni...

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 of ...

The anterior cingulate cortex (ACC) is an important brain area for the regulation of neuropathic pain. The α2A adrenoceptor is a good target for pain management. However, the role of cingulate α2A adrenoceptors in the regulation of neuropathic pain has been less studied. In this study, we investigated the involvement of cingulate α2A adrenoceptors in the regulation of neuropathic pain at differ...

1. The subtype and anatomical localization of beta-adrenoceptors mediating facilitation of stimulus-induced overflow of noradrenaline ('prejunctional beta-adrenoceptors') are not conclusively known to date. The present study was undertaken to characterize these receptors by use of pharmacological methods as well as to define their localization (prejunctional or postjunctional) with radio-ligand...

BACKGROUND AND PURPOSE β(1) -, β(2) - and β(3) -adrenoceptors determined by functional, binding and reverse transcription polymerase chain reaction (RT-PCR) studies are present in chick astrocytes and activation of β(2) - or β(3) -adrenoceptors increase glucose uptake. The aims of the present study are to identify which β-adrenoceptor subtypes are present in mouse astrocytes, the signal transdu...

Benign prostatic hyperplasia (BPH), common in aging males, is often treated with alpha(1)-adrenoceptor antagonists. To minimize hypotensive and other side effects, compounds with selective antagonist activity at alpha(1A)- and alpha(1D)- (compared with alpha(1B)-) adrenoceptors were evaluated that would block lower urinary tract alpha(1)-adrenoceptors in preference to cardiovascular alpha(1B)-a...