Posted by SLS on April 2, 2010, at 7:15:48
In reply to Re: - Interesting Antipsychotic, posted by SLS on April 1, 2010, at 19:02:07
Here's the one that I couldn't find the other day.
- Scott
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Eur J Pharmacol. 2003 Feb 21;462(1-3):33-40.
alpha2C-Adrenoceptor blockade by clozapine and other antipsychotic drugs.Kalkman HO, Loetscher E.
Novartis Pharma AG, Research Nervous System, Building WSJ-360-405, CH-4002 Basel, Switzerland. hans.kalkman@pharma.novartis.com
The noradrenergic system may play a role in antipsychotic modulation of schizophrenia symptoms. Therefore, the antagonistic potencies of the antipsychotics clozapine, chlorpromazine, risperidone, olanzapine, haloperidol, quetiapine, ziprasidone, iloperidone and aripiprazole were quantified using cell lines expressing the recombinant human alpha(2C)-adrenoceptor, alpha(2A)-adrenoceptor, or dopamine D(2L) receptor. The alpha(2)-adrenoceptor antagonists, yohimbine and idazoxan, were also tested. Alterations in cAMP were measured as changes in luminescence. In the alpha(2A)-adrenoceptor cell line, the agonist 5-bromo-6-(2-imidazolin-2-ylamino)quinoxaline (UK14,304) induced a concentration-dependent increase in luminescence. In cell lines expressing alpha(2C) and D(2L) receptors, agonists induced a concentration-dependent reduction in luminescence. Yohimbine and idazoxan were the most potent alpha(2A)-adrenoceptor antagonists, yohimbine and iloperidone were the most potent alpha(2C)-adrenoceptor antagonists, and haloperidol and olanzapine were the most potent dopamine D(2) receptor antagonists. Clozapine had the highest alpha(2C)/D(2) selectivity, and iloperidone the highest alpha(2C)/alpha(2A) ratio. It is hypothesised that alpha(2C)-adrenoceptor blockade contributes to improvement of cognitive function.
poster:SLS
thread:939163
URL: http://www.dr-bob.org/babble/neuro/20100223/msgs/941754.html