Seroquel® (Quetiapine Hemifumarate)
27 Oct 2010-pp 129-163
About: The article was published on 2010-10-27. It has received None citations till now.
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TL;DR: The data strongly suggest that the antidepressant activity of quetiapine is mediated, at least in part, by its metabolite N-DesalkylquetiAPine through NET inhibition and partial 5-HT1A agonism.
297 citations
TL;DR: Dyskinetic clozapine is a low-potency D2 dopamine receptor antagonist which appears to act selectively in the mesolimbic area and initial examination of a few close cogeners of 1 enhanced confidence in the Cebus model as a predictor of dyskinetic potential.
Abstract: A great need exists for antipsychotic drugs which will not induce extrapyramidal symptoms (EPS) and tardive dyskinesias (TDs) These side effects are deemed to be a consequence of nonselective blockade of nigrostriatal and mesolimbic dopamine D2 receptors Nondyskinetic clozapine (1) is a low-potency D2 dopamine receptor antagonist which appears to act selectively in the mesolimbic area In this work dopamine antagonism was assessed in two mouse behavioral assays: antagonism of apomorphine-induced climbing and antagonism of apomorphine-induced disruption of swimming The potential for the liability of dyskinesias was determined in haloperidol-sensitized Cebus monkeys Initial examination of a few close cogeners of 1 enhanced confidence in the Cebus model as a predictor of dyskinetic potential Considering dibenzazepines, 2 was not dyskinetic whereas 2a was dyskinetic Among dibenzodiazepines, 1 did not induce dyskinesias whereas its N-2-(2-hydroxyethoxy)ethyl analogue 3 was dyskinetic The emergence of such distinctions presented an opportunity Thus, aromatic and N-substituted analogues of 6-(piperazin-1-yl)-11H-dibenz[b,e]azepines and 11-(piperazin-1-yl)dibenzo[b,f][1,4]thiazepines and -oxazepines were prepared and evaluated 11-(4-[2-(2-Hydroxyethoxy)ethyl]piperazin-1-yl)dibenzo[b,f][1,4]thiazepine (23) was found to be an apomorphine antagonist comparable to clozapine It was essentially nondyskinetic in the Cebus model With 23 as a platform, a number of N-substituted analogues were found to be good apomorphine antagonists but all were dyskinetic
73 citations
TL;DR: In this article, a homotopic 1,10-diaza-18-crown-6 derivatives with two, four, and six chiral centers have been prepared in optically active form from diethanolamines via a cyclization reaction with tosylates 39 and 48.
Abstract: Homotopic 1,10-diaza-18-crown-6 derivatives with two, four, and six chiral centers have been prepared in optically active form from diethanolamines via a cyclization reaction with tosylates 39 and 48. The requisite optically active diethanolamines were prepared from chiral cyanohydrins and chiral ethanolamines by a one-pot Grignard-transimination-reduction or a one-pot reduction-transimination-reduction procedure. Yields were strongly affected by the size of the substituents α to the nitrogen atom. The stereoselectivity of the diethanolamine synthesis was found to depend on the configuration of the ethanolamine used
41 citations
TL;DR: In this paper, an intramolecular application of LEUCKART's amide synthesis using isocyanato-diphenylsulphides, -diphensyloxides, and -methanes with AlCl3 in o-dichlorobenzene has been found which gives in very good yields 10,11-dihydro-11-oxo-dibenz[b,f]-1,4-thiazepines (VII), -oxazepines (VIII), and 5,6-D
Abstract: By intramolecular application of LEUCKART's amide synthesis using isocyanato-diphenylsulphides, -diphenyloxides and -diphenylmethanes with AlCl3 in o-dichlorobenzene a method has been found which gives in very good yields 10,11-dihydro-11-oxo-dibenz[b,f]-1,4-thiazepines (VII), -oxazepines (VIII), and 5,6-Dihydro-6-oxo-dibenz[b,e]-azepines (XI), respectively.
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29 citations