Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding

…, AS Lesage, K De Loore, JE Leysen - …, 1996 - Springer
Risperidone and its active metabolite 9-OH-risperidone were compared to reference
antipsychotic drugs (haloperidol, pipamperone, fluspirilene, clozapine, zotepine) and compounds …

[PDF][PDF] Biochemical profile of risperidone, a new antipsychotic.

JE Leysen, W Gommeren, A Eens… - … of Pharmacology and …, 1988 - Citeseer
Materials and Methods Radioligand receptor binding and neurotransmitter uptake assays:
inhibition by drugs Female Wistar rats (150 g) or male Pirbright guinea pigs (200 g) were …

Receptor-binding properties in vitro and in vivo of ritanserin: A very potent and long acting serotonin-S2 antagonist.

JE Leysen, W Gommeren, P Van Gompel… - Molecular …, 1985 - ASPET
In vitro and in vivo receptor-binding properties of the new serotonin antagonist, ritanserin,
are reported. In in vitro binding assays, ritanserin shows high affinity binding to serotonin-S2 …

Serotonergic component of neuroleptic receptors

JE Leysen, CJE Niemegeers, JP Tollenaere… - Nature, 1978 - nature.com
BINDING studies performed in vitro with 3 H-haloperidol 1–3 , 3 H-spiperone 4–5 , 3 H-dopamine
1–3,6 and 3 H-apomorphine 7,8 showed that the specific neuroleptic binding sites in …

5-HT2 receptors

JE Leysen - Current Drug Targets-CNS & Neurological …, 2004 - ingentaconnect.com
5-HT2 receptors are G-protein coupled receptors that currently comprise threesubtypes: 5-HT2A,
5-HT2B and 5-HT2C receptors. The subtypes are related in theirmolecular structure, …

Risperidone: a novel antipsychotic with balanced serotonin-dopamine antagonism, receptor occupancy profile, and pharmacologic activity.

JE Leysen, PM Janssen, AA Megens… - The Journal of clinical …, 1994 - europepmc.org
The interaction of risperidone, 9-hydroxyrisperidone (the principal active metabolite), and
clozapine with neurotransmitter receptors was investigated in vitro using animal brain tissue …

Receptor binding profile of R 41 468, a novel antagonist at 5-HT2 receptors

JE Leysen, F Awouters, L Kennis, PM Laduron… - Life sciences, 1981 - Elsevier
For a new antiserotonergic agent, R 41 468 and 13 reference compounds with alleged
antiserotonergic activity, the receptor binding profile is reported, comprising K i -values measured …

Interaction of antipsychotic drugs with neurotransmitter receptor sites in vitro and in vivo in relation to pharmacological and clinical effects: role of 5HT2 receptors

JE Leysen, PMF Janssen, A Schotte, WHML Luyten… - …, 1993 - Springer
… uptake models was measured in radioligand binding assays using tissue homogenates or
membrane preparations of cells expressing cloned receptors as described in Leysen et al. (…

5-HT2A and 5-HT2C receptors and their atypical regulation properties

D Van Oekelen, WHML Luyten, JE Leysen - Life sciences, 2003 - Elsevier
The 5-HT 2A and 5-HT 2C receptors belong to the G-protein-coupled receptor (GPCR)
superfamily. GPCRs transduce extracellular signals to the interior of cells through their interaction …

Domperidone, a specific in vitro dopamine antagonist, devoid of in vivo central dopaminergic activity

PM Laduron, JE Leysen - Biochemical pharmacology, 1979 - Elsevier
When tested in different in vitro binding assays and in dopamine-sensitive adenylate cyclase,
domperidone was found to be a very potent and specifie dopamine antagonist. Accordingly…