Journal ArticleDOI
Antagonism by neuroleptics of neurotransmitter receptors of normal human brain in vitro.
TLDR
Using radioligand binding techniques, the equilibrium dissociation constants (KD's) for a series of neuroleptics at the dopamine, muscarinic, histamine H1, alpha 1- and alpha 2-adrenergic receptors of normal human brain tissue obtained at autopsy were determined.About:
This article is published in European Journal of Pharmacology.The article was published on 1984-08-17. It has received 213 citations till now. The article focuses on the topics: Spiperone & Molindone.read more
Citations
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Dopamine receptors and the dopamine hypothesis of schizophrenia.
TL;DR: Direct evidence that neuroleptics selectively blocked dopamine receptors occurred in 1974 with the finding that nanomolar concentrations of these drugs stereoselectively inhibited the binding of [3H]‐dopamine or [3h]‐haloperidol.
Journal ArticleDOI
Polymorphism of human cytochrome P450 enzymes and its clinical impact
TL;DR: Current pharmacogenetic knowledge on important human drug-metabolizing cytochrome P450s (CYPs) is highlighted to understand the large interindividual variability in drug clearance and responses in clinical practice and to improve the efficacy and safety of both prospective and currently available drugs.
Journal ArticleDOI
Clozapine. A novel antipsychotic agent.
TL;DR: This review considers the discovery of clozapine; its chemistry, pharmacologic activities, metabolism, and pharmacokinetics; evidence of its efficacy; and its side effects and appropriate clinical use.
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Schizophrenia, just the facts: What do we know, how well do we know it?
TL;DR: The basic facts of schizophrenia are subjectively reviewed in terms of their reproducibility and significance for understanding the disorder.
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Clinical and biologic response to clozapine in patients with schizophrenia. Crossover comparison with fluphenazine.
David Pickar,Richard R. Owen,Robert E. Litman,P. Eric Konicki,Rolando Gutierrez,Mark Hyman Rapaport +5 more
TL;DR: Clozapine significantly reduced total as well as positive and negative symptoms in comparison with both fluphenazine and placebo, and eight patients (38%) showed CLZAPINE superiority on the basis of prospective response criteria as discussed by the authors.
References
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Ligand: a versatile computerized approach for characterization of ligand-binding systems.
Peter J. Munson,David Rodbard +1 more
TL;DR: This approach provides two major advantages compared with other available methods: it uses an exact mathematical model of the ligand-binding system, thereby avoiding the possible biases introduced by several commonly used approximations and it uses a statistically valid, appropriately weighted least-squares curve-fitting algorithm with objective measurement of goodness of fit.
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Dopamine receptor binding predicts clinical and pharmacological potencies of antischizophrenic drugs
TL;DR: Clinical potencies of butyrophenones, phenothiazines, and related drugs correlate closely with their ability to inhibit tritiated haloperidol binding, providing a simple in vitro means for evaluating new drugs as potential antischizophrenic agents.
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Antipsychotic drug doses and neuroleptic/dopamine receptors
TL;DR: It is reported here that all clinically effective antipsychotic drugs (tested so far) block the stereo-specific binding of 3H-haloperidol at concentrations which correlate directly with the clinical potencies.
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Relationship of neuroleptic drug effects at brain dopamine, serotonin, alpha-adrenergic, and histamine receptors to clinical potency.
Peroutka Sj,Synder Sh +1 more
TL;DR: The authors examined the potencies of 22 neuroleptic drugs competing for binding sites associated with dopamine, serotonin, alpha-adrenergic, and histamine receptors in brain membranes and found that although many neuroleptics are quite potent in competing at several receptor sites, the average antipsychotic clinical potency correlates closely only with the drug affinity for dopamine receptors labeled by 3H-spiroperidol.
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3H-spiroperidol labels dopamine receptors in pituitary and brain
TL;DR: 3H-Spiroperidol of high specific radioactivity labels dopamine receptors in membranes of bovine caudate nucleus and anterior pituitary and shows very high affinity with a dissociation constant of 0.2-0.3 nM.