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1988 6
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7-[3-(4-[2,3-Dimethylphenyl]piperazinyl)propoxy]-2(1H)-quinolinone (OPC-4392), a presynaptic dopamine autoreceptor agonist and postsynaptic D2 receptor antagonist.
Yasuda Y, Kikuchi T, Suzuki S, Tsutsui M, Yamada K, Hiyama T. Yasuda Y, et al. Life Sci. 1988;42(20):1941-54. doi: 10.1016/0024-3205(88)90493-6. Life Sci. 1988. PMID: 3130534
The assertion that OPC-4392 acts as an agonist at presynaptic dopamine autoreceptors is supported by the following behavioral and biochemical observations: OPC-4392, 3-PPP and apomorphine inhibited the reserpine-induced increase in DOPA accumulation in …
The assertion that OPC-4392 acts as an agonist at presynaptic dopamine autoreceptors is supported by the following behavioral …
Effect of 7-(3-[4-(2,3-dimethylphenyl)piperazinyl]propoxy)- 2(1H)-quinolinone (OPC-4392), a newly synthesized agonist for presynaptic dopamine D2 receptor, on tyrosine hydroxylation in rat striatal slices.
Kiuchi K, Hirata Y, Minami M, Nagatsu T. Kiuchi K, et al. Life Sci. 1988;42(3):343-9. doi: 10.1016/0024-3205(88)90644-3. Life Sci. 1988. PMID: 2892110
OPC-4392 dose-dependently inhibited L-dihydroxyphenylalanine (DOPA) formation in rat striatal slices with IC50 values of about 10(-6) M. ...From in vitro experiment using purified TH, OPC-4392 affected neither the enzymatic activity nor the Km value fo …
OPC-4392 dose-dependently inhibited L-dihydroxyphenylalanine (DOPA) formation in rat striatal slices with IC50 values of about …
Phase 1 study of a new antipsychotic drug, OPC-4392.
Murasaki M, Miura S, Ishigooka J, Ishii Y, Takahashi A, Fukuyama Y. Murasaki M, et al. Prog Neuropsychopharmacol Biol Psychiatry. 1988;12(5):793-802. doi: 10.1016/0278-5846(88)90024-3. Prog Neuropsychopharmacol Biol Psychiatry. 1988. PMID: 2906159
1. A phase I study of OPC-4392 (OPC), a quinolinone derivative recently developed in Japan and recognized to have an agonistic effect on dopamine autoreceptors, was performed in 7 male healthy volunteers in comparison with chlorpromazine (CPZ). 2. ...Pharmacokinetic …
1. A phase I study of OPC-4392 (OPC), a quinolinone derivative recently developed in Japan and recognized to have an agonistic …
Presynaptic inhibition of excitatory input from the substantia nigra to caudate nucleus neurons by a substituted quinolinone derivative, 7-[3-(4-(2,3-dimethylphenyl)piperazinyl)propoxy]-2(1H)-quinolinone (OPC-4392).
Sasa M, Ohno Y, Takaori S. Sasa M, et al. Life Sci. 1988;43(3):263-9. doi: 10.1016/0024-3205(88)90316-5. Life Sci. 1988. PMID: 3398698
In addition, OPC-4392 did not inhibit firing induced by bromocriptine, a dopamine D-2 agonist; while domperidone suppressed the bromocriptine-induced firing without affecting the glutamate-induced firing. These results suggest that OPC-4392 acts on the …
In addition, OPC-4392 did not inhibit firing induced by bromocriptine, a dopamine D-2 agonist; while domperidone suppressed th …
Neuroendocrine profile of SDZ HDC-912 and OPC-4392, two new atypical antipsychotic drugs, in schizophrenic patients.
Duval F, Mokrani MC, Macher JP, Crocq MA, Castro JO, Bailey P, Lataste X. Duval F, et al. Psychopharmacology (Berl). 1993;110(1-2):177-80. doi: 10.1007/BF02246969. Psychopharmacology (Berl). 1993. PMID: 7870880 Clinical Trial.
The aim of this study was to evaluate the effect on the activity of the hypothalamic-pituitary dopaminergic system of two new atypical antipsychotic drugs: the ergoline derivative SDZ HDC-912, which is a dopamine (DA) D2 receptor partial agonist; and the quinolinone derivative …
The aim of this study was to evaluate the effect on the activity of the hypothalamic-pituitary dopaminergic system of two new atypical antip …
D-2 receptor-mediated inhibition by a substituted quinolinone derivative, 7-[3-(4-(2,3-dimethylphenyl)piperazinyl)propoxy]-2(1H)-quinolinone (OPC-4392), of dopaminergic neurons in the ventral tegmental area.
Momiyama T, Sasa M, Takaori S. Momiyama T, et al. Life Sci. 1990;47(9):761-9. doi: 10.1016/0024-3205(90)90548-6. Life Sci. 1990. PMID: 1977066
However, in 16 out of 19 type II neurons the antidromic spikes were not affected by either OPC-4392 or dopamine. When the effects of iontophoretically applied OPC-4392 and dopamine on spontaneous firings were tested in 32 VTA neurons identified by Acc …
However, in 16 out of 19 type II neurons the antidromic spikes were not affected by either OPC-4392 or dopamine. When the effe …
Dopamine agonists in schizophrenia: a review.
Benkert O, Müller-Siecheneder F, Wetzel H. Benkert O, et al. Eur Neuropsychopharmacol. 1995;5 Suppl:43-53. doi: 10.1016/0924-977x(95)00022-h. Eur Neuropsychopharmacol. 1995. PMID: 8775758 Review.
Dopamine autoreceptor agonists like pramipexole, roxindole, talipexole and OPC-4392 as well as partial agonists like terguride and SDZ HDC 912 have been tested in positive schizophrenic symptomatology in order to reduce the postulated excess of central dopaminergic …
Dopamine autoreceptor agonists like pramipexole, roxindole, talipexole and OPC-4392 as well as partial agonists like terguride …
[Pharmacology of antipsychotics at human dopamine D2 and D3 receptors].
Tadori Y, Kikuchi T. Tadori Y, et al. Nihon Shinkei Seishin Yakurigaku Zasshi. 2012 Feb;32(1):9-18. Nihon Shinkei Seishin Yakurigaku Zasshi. 2012. PMID: 22568121 Review. Japanese.
Aripiprazole's intrinsic activities at D2 and D9 receptors were lower than those observed with partial agonists (terguride, bifeprunox, OPC-4392 and (-)-3-PPP), which demonstrated clinically suboptimal improvement of positive symptoms of schizophrenia patients, and …
Aripiprazole's intrinsic activities at D2 and D9 receptors were lower than those observed with partial agonists (terguride, bifeprunox, O …
7-(4-[4-(2,3-Dichlorophenyl)-1-piperazinyl]butyloxy)-3,4-dihydro-2(1H)-quinolinone (OPC-14597), a new putative antipsychotic drug with both presynaptic dopamine autoreceptor agonistic activity and postsynaptic D2 receptor antagonistic activity.
Kikuchi T, Tottori K, Uwahodo Y, Hirose T, Miwa T, Oshiro Y, Morita S. Kikuchi T, et al. J Pharmacol Exp Ther. 1995 Jul;274(1):329-36. J Pharmacol Exp Ther. 1995. PMID: 7616416
The effects of 7-(4-[4-(2,3-dichlorophenyl)-1-piperazinyl]butyloxy)-3,4-dihydro-2 (1H)- quinolinone (OPC-14597), a derivative of the dopamine (DA) autoreceptor agonist 7-(3-[4-(2,3-dimethylphenyl)piperazinyl]propoxy)-2(1H)-quinolinone (OPC-4392), on DA receptors wer …
The effects of 7-(4-[4-(2,3-dichlorophenyl)-1-piperazinyl]butyloxy)-3,4-dihydro-2 (1H)- quinolinone (OPC-14597), a derivative of the dopamin …
21 results