| Publication |
Sentence |
Publish Date |
Extraction Date |
Species |
| H J Möller, E Pelzer, W Kissling, T Riehl, T Wernick. Efficacy and tolerability of a new antipsychotic compound (risperidone): results of a pilot study. Pharmacopsychiatry. vol 24. issue 6. 1992-06-10. PMID:1725925. |
risperidone is a new benzisoxazole derivative displaying a very potent serotonin antagonism and a potent dopamine antagonism in pharmacological studies. |
1992-06-10 |
2023-08-11 |
Not clear |
| J E Leysen, P M Janssen, W Gommeren, J Wynants, P J Pauwels, P A Jansse. In vitro and in vivo receptor binding and effects on monoamine turnover in rat brain regions of the novel antipsychotics risperidone and ocaperidone. Molecular pharmacology. vol 41. issue 3. 1992-04-16. PMID:1372084. |
further, the drugs bound at nanomolar concentrations to the following receptors (ki values, in nm, for ocaperidone and risperidone, respectively): alpha 1-adrenergic (0.46 and 0.81), dopamine d2 (0.75 and 3.0), histamine h1 (1.6 and 2.1), and alpha 2-adrenergic (5.4 and 7.3). |
1992-04-16 |
2023-08-11 |
human |
| J E Leysen, P M Janssen, W Gommeren, J Wynants, P J Pauwels, P A Jansse. In vitro and in vivo receptor binding and effects on monoamine turnover in rat brain regions of the novel antipsychotics risperidone and ocaperidone. Molecular pharmacology. vol 41. issue 3. 1992-04-16. PMID:1372084. |
ocaperidone, risperidone, and haloperidol readily increased the levels of the dopamine metabolites 3,4-dihydroxybenzene acetic acid and homovanillic acid in the striatum, the nucleus accumbens, the tuberculum olfactorium, and, to some extent, the frontal cortex. |
1992-04-16 |
2023-08-11 |
human |
| A A Megens, F H Awouters, T F Meert, K H Schellekens, C J Niemegeers, P A Jansse. Pharmacological profile of the new potent neuroleptic ocaperidone (R 79,598). The Journal of pharmacology and experimental therapeutics. vol 260. issue 1. 1992-02-18. PMID:1370538. |
ocaperidone inhibited dopamine agonist (apomorphine, amphetamine or cocaine)-induced behavioral effects at low doses (0.014-0.042 mg/kg) and was, thereby, equipotent with haloperidol (0.016-0.024 mg/kg) and 2.0 to 8.3 times more potent than risperidone. |
1992-02-18 |
2023-08-11 |
Not clear |
| A A Megens, F H Awouters, T F Meert, K H Schellekens, C J Niemegeers, P A Jansse. Pharmacological profile of the new potent neuroleptic ocaperidone (R 79,598). The Journal of pharmacology and experimental therapeutics. vol 260. issue 1. 1992-02-18. PMID:1370538. |
ocaperidone completely blocked the dopamine agonist behavior at slightly higher doses (0.064 mg/kg) and was, thereby, more potent and efficacious than haloperidol (0.097-0.13 mg/kg) and risperidone (0.59-1.17 mg/kg). |
1992-02-18 |
2023-08-11 |
Not clear |
| A A Megens, F H Awouters, T F Meert, K H Schellekens, C J Niemegeers, P A Jansse. Pharmacological profile of the new potent neuroleptic ocaperidone (R 79,598). The Journal of pharmacology and experimental therapeutics. vol 260. issue 1. 1992-02-18. PMID:1370538. |
ocaperidone displayed its serotonin and dopamine antagonism at the same dose levels, in contrast to risperidone, which was a predominant serotonin antagonist. |
1992-02-18 |
2023-08-11 |
Not clear |
| J Bergman, B K Madras, R D Spealma. Behavioral effects of D1 and D2 dopamine receptor antagonists in squirrel monkeys. The Journal of pharmacology and experimental therapeutics. vol 258. issue 3. 1991-10-17. PMID:1890625. |
d2-selective antagonists included cis-n-(1-benzyl-2-methylpyrrolidine-3-yl)-5-chloro-2-methoxy-4- methylaminobenzamide, ym-09151-2, eticlopride, raclopride, haloperidol, risperidone, remoxipride, s-sulpiride and r-sulpiride; nonselective dopamine antagonists were s-butaclamol and chlorpromazine. |
1991-10-17 |
2023-08-11 |
monkey |
| M B Bogdanov, R R Gaĭnetdinov, V S Kudrin, O S Medvedev, A V Val'dma. [Study by the intracerebral microdialysis method of the effects of atypical neuroleptics and anxiolytics on striatal release and metabolism of dopamine in awake rats]. Biulleten' eksperimental'noi biologii i meditsiny. vol 111. issue 5. 1991-10-03. PMID:1715214. |
using brain microdialysis in awake rats effects of risperidone, ritanserin, buspirone, sulpiride and 5-methoxy-n,n-dimethyltryptamine (meodmt) on striatal dopamine (da) release and metabolism were studied. |
1991-10-03 |
2023-08-11 |
rat |
| P Seema. Atypical neuroleptics: role of multiple receptors, endogenous dopamine, and receptor linkage. Acta psychiatrica Scandinavica. Supplementum. vol 358. 1990-12-14. PMID:1978482. |
although dopamine d2 receptor blockade continues to be a dominant feature of successful neuroleptics, the concomitant blockade of muscarinic or serotonergic s2 receptors helps to prevent neuroleptic-induced parkinsonism for some atypical neuroleptics (clozapine, thioridazine, risperidone). |
1990-12-14 |
2023-08-11 |
Not clear |
| C J Niemegeers, F Awouters, P A Jansse. [Serotonin antagonism involved in the antipsychotic effect. Confirmation with ritanserine and risperidone]. L'Encephale. vol 16. issue 2. 1990-07-18. PMID:1693560. |
these properties, being valuable by themselves, have been associated to dopamine d2-antagonism in the new antipsychotic risperidone, which is an extremely potent 5-ht2-antagonist. |
1990-07-18 |
2023-08-11 |
Not clear |
| A Schotte, K de Bruyckere, P F Janssen, J E Leyse. Receptor occupancy by ritanserin and risperidone measured using ex vivo autoradiography. Brain research. vol 500. issue 1-2. 1990-02-20. PMID:2481562. |
in this study, autoradiographical techniques are introduced to investigate the occupancy of serotonin 5-ht2, dopamine d2 and alpha 1-adrenergic receptors after the in vivo administration of ritanserin, a selective, potent and long-acting 5-ht2 antagonist and of risperidone, a very potent 5-ht2 antagonist and potent d2 and alpha 1 antagonist. |
1990-02-20 |
2023-08-11 |
rat |
| J E Leysen, W Gommeren, A Eens, D de Chaffoy de Courcelles, J C Stoof, P A Jansse. Biochemical profile of risperidone, a new antipsychotic. The Journal of pharmacology and experimental therapeutics. vol 247. issue 2. 1988-12-21. PMID:2460616. |
risperidone did not affect the activation by amphetamine of [3h]dopamine efflux from rat striatal slices. |
1988-12-21 |
2023-08-11 |
human |