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• W201215393 abstract "i Title: Characterisation of the uu-adrenoceptor antagonism by mirtazapine and its modifying effects on receptor signalling Mirtazapine is an atypical antidepressant employed clinically for the treatment of major depression. As a multipotent antagonist it acts at am-adrenergic receptors (%-ARs). serotonin type-2A receptors (SHTm-Rs) and histamine type-I receptors (H,-Rs). Its actions at the amAR have been proposed to play a role in its putative earlier onset of action. However, it is not known whether mirtazapine is a neutral antagonist or inverse agonist at azARs. The current study aimed to determine the mode of am-AR antagonism by mirtazapine, as well as to investigate in vitro the modulatory effects of mirtazapine pre-treatments on padrenergic receptor (PAR), muscarinic acetylcholine receptor (mAChR) and auAR functions. Chinese hamster ovary (CHO-K1) cells expressing the porcine am-AR at high numbers (%AH), a constitutively active mutant am-AR (%-CAM), or mock-transfected control cells (neo) were radio-labelled with [3H]-adenine and concentration-effect curves of mirtazapine, yohimbine, mianserin or idazoxan were constructed, measuring [3H]-cA~P accumulation. In addition human neuroblastoma SH-SY5Y cells and CHO-K1 cells expressing the porcine amAR at low numbers (am-L) were used to investigate the effect of mirtazapine pre-treaments on mAChRs and PARS or am-ARs respectively. ARer radio-labelling with myo-[2-3H]-inositol or [2-%]-adenine, radio-label uptake was measured and receptor function was investigated by constructing concentration-effect curves, measuring [3~] -1~, or [ 3 ~ ] c A ~ ~ accumulation respectively. The results from the current study show that mirtazapine binds to the am-AR with an affinity value in the lower micromolar range (K, .; 0.32 pM; pK, = 6.50 + 0.07). Mirtazapine is not a partial agonist at am-ARs as it does not affect [ 3 H ] c A ~ ~ accumulation in am-H cells. Preliminary results suggest that mirtazapine displays partial inverse agonism in Q-CAM cells, while mianserin displays neutral antagonism. Mirtazapine pretreatment in SH-SY5Y cells does not alter muscarinic receptor function (different from fluoxetine and imipramine), but reduces Cisoproterenol-induced increase in [3H]-cAM~ accumulation in SH-SY5Y cells" @default.
• W201215393 created "2016-06-24" @default.
• W201215393 creator A5050663168 @default.
• W201215393 date "2004-01-01" @default.
• W201215393 modified "2023-09-24" @default.
• W201215393 title "Characterisation of the ?2A-adrenoceptor antagonism by mirtazapine and its modifying effects on receptor signalling" @default.
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