Publication |
Sentence |
Publish Date |
Extraction Date |
Species |
Fuji Yokoi, Gerhard Gründer, Kathleen Biziere, Massoud Stephane, Ahmet S Dogan, Robert F Dannals, Hayden Ravert, Ajit Suri, Steven Bramer, Dean F Won. Dopamine D2 and D3 receptor occupancy in normal humans treated with the antipsychotic drug aripiprazole (OPC 14597): a study using positron emission tomography and [11C]raclopride. Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology. vol 27. issue 2. 2002-08-07. PMID:12093598. |
dopamine d2 and d3 receptor occupancy in normal humans treated with the antipsychotic drug aripiprazole (opc 14597): a study using positron emission tomography and [11c]raclopride. |
2002-08-07 |
2023-08-12 |
human |
Fuji Yokoi, Gerhard Gründer, Kathleen Biziere, Massoud Stephane, Ahmet S Dogan, Robert F Dannals, Hayden Ravert, Ajit Suri, Steven Bramer, Dean F Won. Dopamine D2 and D3 receptor occupancy in normal humans treated with the antipsychotic drug aripiprazole (OPC 14597): a study using positron emission tomography and [11C]raclopride. Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology. vol 27. issue 2. 2002-08-07. PMID:12093598. |
aripiprazole (opc 14597) is an antipsychotic drug that has high affinity for dopamine d2 and d3 receptors and the dopamine autoreceptor. |
2002-08-07 |
2023-08-12 |
human |
Fuji Yokoi, Gerhard Gründer, Kathleen Biziere, Massoud Stephane, Ahmet S Dogan, Robert F Dannals, Hayden Ravert, Ajit Suri, Steven Bramer, Dean F Won. Dopamine D2 and D3 receptor occupancy in normal humans treated with the antipsychotic drug aripiprazole (OPC 14597): a study using positron emission tomography and [11C]raclopride. Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology. vol 27. issue 2. 2002-08-07. PMID:12093598. |
the purpose of this study was to determine whether a dose response following graduated doses of aripiprazole could be quantified and correlated with its occupancy of the d2 and d3 dopamine receptors in the brain of living humans. |
2002-08-07 |
2023-08-12 |
human |
Kevin D Burris, Thaddeus F Molski, Cen Xu, Elaine Ryan, Katsura Tottori, Tetsuro Kikuchi, Frank D Yocca, Perry B Molinof. Aripiprazole, a novel antipsychotic, is a high-affinity partial agonist at human dopamine D2 receptors. The Journal of pharmacology and experimental therapeutics. vol 302. issue 1. 2002-07-12. PMID:12065741. |
aripiprazole, a novel antipsychotic, is a high-affinity partial agonist at human dopamine d2 receptors. |
2002-07-12 |
2023-08-12 |
human |
Kevin D Burris, Thaddeus F Molski, Cen Xu, Elaine Ryan, Katsura Tottori, Tetsuro Kikuchi, Frank D Yocca, Perry B Molinof. Aripiprazole, a novel antipsychotic, is a high-affinity partial agonist at human dopamine D2 receptors. The Journal of pharmacology and experimental therapeutics. vol 302. issue 1. 2002-07-12. PMID:12065741. |
consistent with the expected effects of a partial agonist, increasing concentrations of aripiprazole blocked the action of dopamine with maximal blockade equal to the agonist effect of aripiprazole alone. |
2002-07-12 |
2023-08-12 |
human |
Kevin D Burris, Thaddeus F Molski, Cen Xu, Elaine Ryan, Katsura Tottori, Tetsuro Kikuchi, Frank D Yocca, Perry B Molinof. Aripiprazole, a novel antipsychotic, is a high-affinity partial agonist at human dopamine D2 receptors. The Journal of pharmacology and experimental therapeutics. vol 302. issue 1. 2002-07-12. PMID:12065741. |
the efficacy of aripiprazole relative to that of dopamine varied from 25% in cells that lacked spare receptors for dopamine to 90% in cells with receptor reserve. |
2002-07-12 |
2023-08-12 |
human |
C A Tamming. Partial dopamine agonists in the treatment of psychosis. Journal of neural transmission (Vienna, Austria : 1996). vol 109. issue 3. 2002-05-23. PMID:11956961. |
moreover, now a partial dopamine agonist, aripiprazole, has been developed and will likely be marketed by bms and otsuka for the treatment of psychosis and will be the first drug in this class to be commercially available. |
2002-05-23 |
2023-08-12 |
Not clear |
S M Stah. Dopamine system stabilizers, aripiprazole, and the next generation of antipsychotics, part 1, "Goldilocks" actions at dopamine receptors. The Journal of clinical psychiatry. vol 62. issue 11. 2002-03-06. PMID:11775041. |
dopamine system stabilizers, aripiprazole, and the next generation of antipsychotics, part 1, "goldilocks" actions at dopamine receptors. |
2002-03-06 |
2023-08-12 |
Not clear |
J A Schetz, D R Sible. Tandem sulfur-containing amino acids are epicritical determinants of dopamine D(2) receptor pharmacology. European journal of pharmacology. vol 388. issue 2. 2000-03-16. PMID:10666514. |
while previous point mutation studies did not reveal any single one of these residues as being critical for ligand binding, we now show that simultaneously substituting all three with isovolumetric, non sulfur-containing amino acids results in large decreases in the binding affinity for dopamine, (-)-raclopride and 7-(-4(4-(2, 3-dichlorophenyl)-1-piperazinyl)butyloxy)-3, 4-dihydro-2(1h)-quinolinone (aripiprazole), but not for methylspiperone or allosteric modulators. |
2000-03-16 |
2023-08-12 |
Not clear |
H Matsubayashi, T Amano, M Sas. Inhibition by aripiprazole of dopaminergic inputs to striatal neurons from substantia nigra. Psychopharmacology. vol 146. issue 2. 1999-12-02. PMID:10525748. |
aripiprazole (opc-14597) elicits both dopamine d(2) agonist and antagonist activities on dopaminergic neurons of the ventral tegmental area and nucleus accumbens neurons, respectively. |
1999-12-02 |
2023-08-12 |
Not clear |
C P Lawler, C Prioleau, M M Lewis, C Mak, D Jiang, J A Schetz, A M Gonzalez, D R Sibley, R B Mailma. Interactions of the novel antipsychotic aripiprazole (OPC-14597) with dopamine and serotonin receptor subtypes. Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology. vol 20. issue 6. 1999-06-24. PMID:10327430. |
interactions of the novel antipsychotic aripiprazole (opc-14597) with dopamine and serotonin receptor subtypes. |
1999-06-24 |
2023-08-12 |
Not clear |
A Inoue, Y Nakat. [How do antipsychotics exert their effects on dopamine receptor subtypes?]. Nihon yakurigaku zasshi. Folia pharmacologica Japonica. vol 112. issue 6. 1999-05-17. PMID:10202760. |
aripiprazole, a candidate for a novel antipsychotic, has an antagonistic activity against dopamine d2 receptors with a high affinity, but has a weaker potency to up-regulate d2 receptors than haloperidol in the striatum and inhibitory effects on d2-receptor binding activities and mrna in the pituitary, when it is chronically administrated to rats. |
1999-05-17 |
2023-08-12 |
rat |
A Inoue, S Miki, M Seto, T Kikuchi, S Morita, H Ueda, Y Misu, Y Nakat. Aripiprazole, a novel antipsychotic drug, inhibits quinpirole-evoked GTPase activity but does not up-regulate dopamine D2 receptor following repeated treatment in the rat striatum. European journal of pharmacology. vol 321. issue 1. 1997-08-26. PMID:9083792. |
aripiprazole, a novel antipsychotic drug, inhibits quinpirole-evoked gtpase activity but does not up-regulate dopamine d2 receptor following repeated treatment in the rat striatum. |
1997-08-26 |
2023-08-12 |
rat |
A Inoue, S Miki, M Seto, T Kikuchi, S Morita, H Ueda, Y Misu, Y Nakat. Aripiprazole, a novel antipsychotic drug, inhibits quinpirole-evoked GTPase activity but does not up-regulate dopamine D2 receptor following repeated treatment in the rat striatum. European journal of pharmacology. vol 321. issue 1. 1997-08-26. PMID:9083792. |
the effects of chronic administration of aripiprazole and haloperidol on dopamine d2 receptor binding and mrna level in rat striata were examined by a [3h]spiperone binding assay and a ribonuclease protection assay. |
1997-08-26 |
2023-08-12 |
rat |
A Inoue, S Miki, M Seto, T Kikuchi, S Morita, H Ueda, Y Misu, Y Nakat. Aripiprazole, a novel antipsychotic drug, inhibits quinpirole-evoked GTPase activity but does not up-regulate dopamine D2 receptor following repeated treatment in the rat striatum. European journal of pharmacology. vol 321. issue 1. 1997-08-26. PMID:9083792. |
a high dose of aripiprazole (100 mg/kg) only tended to increase the bmax of [3h]spiperone binding non-significantly, and had no effect on the level of dopamine d2l receptor mrna. |
1997-08-26 |
2023-08-12 |
rat |
A Inoue, S Miki, M Seto, T Kikuchi, S Morita, H Ueda, Y Misu, Y Nakat. Aripiprazole, a novel antipsychotic drug, inhibits quinpirole-evoked GTPase activity but does not up-regulate dopamine D2 receptor following repeated treatment in the rat striatum. European journal of pharmacology. vol 321. issue 1. 1997-08-26. PMID:9083792. |
these results indicated that aripiprazole had an antagonistic activity to dopamine d2 receptors with a high affinity, but that the potency of aripiprazole to up-regulate dopamine d2 receptors in the striatum was much smaller than that of haloperidol. |
1997-08-26 |
2023-08-12 |
rat |