The relationship between the daily dose, the plasma concentration of blonanserin, and its plasma anti-dopamine D2 and anti-serotonin 5-HT2A activity
Objective Blonanserin (BNS) possesses anti‐serotonin 5‐HT2A activity in addition to anti‐dopamine D2 activity, which is characteristic of second‐generation antipsychotics, little information is available on its pharmacologic profile in vivo. We investigated the BNS daily dose, plasma concentration,...
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| Published in | Human psychopharmacology Vol. 25; no. 4; pp. 342 - 346 |
|---|---|
| Main Authors | , |
| Format | Journal Article |
| Language | English |
| Published |
Chichester, UK
John Wiley & Sons, Ltd
01.06.2010
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| Subjects | |
| Online Access | Get full text |
| ISSN | 0885-6222 1099-1077 1099-1077 |
| DOI | 10.1002/hup.1124 |
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| Abstract | Objective
Blonanserin (BNS) possesses anti‐serotonin 5‐HT2A activity in addition to anti‐dopamine D2 activity, which is characteristic of second‐generation antipsychotics, little information is available on its pharmacologic profile in vivo. We investigated the BNS daily dose, plasma concentration, plasma anti‐D2 activity, and plasma anti‐5‐HT2A activity in schizophrenia in a total of 14 subjects.
Methods
Blood samples were taken 14 days after the BNS dose was fixed, and the plasma concentration was measured by means of high‐performance liquid chromatographic (HPLC) method. In addition, the plasma anti‐D2 activity and anti‐5‐HT2A activity were measured by means of radioreceptor assays in which [3H]‐spiperone and [3H]‐ketanserin were used.
Results
The results revealed a statistically significant correlation between the daily dose and the plasma concentration (p = 0.04). Statistically significant correlations were also observed between the plasma concentration and the anti‐D2 activity and between the plasma concentration and the anti‐5‐HT2A activity (p = 0.003 and 0.04).
Conclusions
It is therefore believed that both the anti‐D2 activity in plasma and the anti‐5‐HT2A activity in plasma are regulated almost solely by the unchanged principal. Moreover, the mean plasma serotonin/dopamine (S/D) ratio was 0.9 and BNS exhibited both anti‐D2 activity and also anti‐5‐HT2A activity in vivo, as well, so it was clear that the in vitro pharmacological profile was retained in vivo. Copyright © 2010 John Wiley & Sons, Ltd. |
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| AbstractList | Objective
Blonanserin (BNS) possesses anti‐serotonin 5‐HT2A activity in addition to anti‐dopamine D2 activity, which is characteristic of second‐generation antipsychotics, little information is available on its pharmacologic profile in vivo. We investigated the BNS daily dose, plasma concentration, plasma anti‐D2 activity, and plasma anti‐5‐HT2A activity in schizophrenia in a total of 14 subjects.
Methods
Blood samples were taken 14 days after the BNS dose was fixed, and the plasma concentration was measured by means of high‐performance liquid chromatographic (HPLC) method. In addition, the plasma anti‐D2 activity and anti‐5‐HT2A activity were measured by means of radioreceptor assays in which [3H]‐spiperone and [3H]‐ketanserin were used.
Results
The results revealed a statistically significant correlation between the daily dose and the plasma concentration (p = 0.04). Statistically significant correlations were also observed between the plasma concentration and the anti‐D2 activity and between the plasma concentration and the anti‐5‐HT2A activity (p = 0.003 and 0.04).
Conclusions
It is therefore believed that both the anti‐D2 activity in plasma and the anti‐5‐HT2A activity in plasma are regulated almost solely by the unchanged principal. Moreover, the mean plasma serotonin/dopamine (S/D) ratio was 0.9 and BNS exhibited both anti‐D2 activity and also anti‐5‐HT2A activity in vivo, as well, so it was clear that the in vitro pharmacological profile was retained in vivo. Copyright © 2010 John Wiley & Sons, Ltd. Blonanserin (BNS) possesses anti-serotonin 5-HT(2A) activity in addition to anti-dopamine D(2) activity, which is characteristic of second-generation antipsychotics, little information is available on its pharmacologic profile in vivo. We investigated the BNS daily dose, plasma concentration, plasma anti-D(2) activity, and plasma anti-5-HT(2A) activity in schizophrenia in a total of 14 subjects. Blood samples were taken 14 days after the BNS dose was fixed, and the plasma concentration was measured by means of high-performance liquid chromatographic (HPLC) method. In addition, the plasma anti-D(2) activity and anti-5-HT(2A) activity were measured by means of radioreceptor assays in which [(3)H]-spiperone and [(3)H]-ketanserin were used. The results revealed a statistically significant correlation between the daily dose and the plasma concentration (p = 0.04). Statistically significant correlations were also observed between the plasma concentration and the anti-D(2) activity and between the plasma concentration and the anti-5-HT(2A) activity (p = 0.003 and 0.04). It is therefore believed that both the anti-D(2) activity in plasma and the anti-5-HT(2A) activity in plasma are regulated almost solely by the unchanged principal. Moreover, the mean plasma serotonin/dopamine (S/D) ratio was 0.9 and BNS exhibited both anti-D(2) activity and also anti-5-HT(2A) activity in vivo, as well, so it was clear that the in vitro pharmacological profile was retained in vivo. Blonanserin (BNS) possesses anti-serotonin 5-HT(2A) activity in addition to anti-dopamine D(2) activity, which is characteristic of second-generation antipsychotics, little information is available on its pharmacologic profile in vivo. We investigated the BNS daily dose, plasma concentration, plasma anti-D(2) activity, and plasma anti-5-HT(2A) activity in schizophrenia in a total of 14 subjects.OBJECTIVEBlonanserin (BNS) possesses anti-serotonin 5-HT(2A) activity in addition to anti-dopamine D(2) activity, which is characteristic of second-generation antipsychotics, little information is available on its pharmacologic profile in vivo. We investigated the BNS daily dose, plasma concentration, plasma anti-D(2) activity, and plasma anti-5-HT(2A) activity in schizophrenia in a total of 14 subjects.Blood samples were taken 14 days after the BNS dose was fixed, and the plasma concentration was measured by means of high-performance liquid chromatographic (HPLC) method. In addition, the plasma anti-D(2) activity and anti-5-HT(2A) activity were measured by means of radioreceptor assays in which [(3)H]-spiperone and [(3)H]-ketanserin were used.METHODSBlood samples were taken 14 days after the BNS dose was fixed, and the plasma concentration was measured by means of high-performance liquid chromatographic (HPLC) method. In addition, the plasma anti-D(2) activity and anti-5-HT(2A) activity were measured by means of radioreceptor assays in which [(3)H]-spiperone and [(3)H]-ketanserin were used.The results revealed a statistically significant correlation between the daily dose and the plasma concentration (p = 0.04). Statistically significant correlations were also observed between the plasma concentration and the anti-D(2) activity and between the plasma concentration and the anti-5-HT(2A) activity (p = 0.003 and 0.04).RESULTSThe results revealed a statistically significant correlation between the daily dose and the plasma concentration (p = 0.04). Statistically significant correlations were also observed between the plasma concentration and the anti-D(2) activity and between the plasma concentration and the anti-5-HT(2A) activity (p = 0.003 and 0.04).It is therefore believed that both the anti-D(2) activity in plasma and the anti-5-HT(2A) activity in plasma are regulated almost solely by the unchanged principal. Moreover, the mean plasma serotonin/dopamine (S/D) ratio was 0.9 and BNS exhibited both anti-D(2) activity and also anti-5-HT(2A) activity in vivo, as well, so it was clear that the in vitro pharmacological profile was retained in vivo.CONCLUSIONSIt is therefore believed that both the anti-D(2) activity in plasma and the anti-5-HT(2A) activity in plasma are regulated almost solely by the unchanged principal. Moreover, the mean plasma serotonin/dopamine (S/D) ratio was 0.9 and BNS exhibited both anti-D(2) activity and also anti-5-HT(2A) activity in vivo, as well, so it was clear that the in vitro pharmacological profile was retained in vivo. Objective Blonanserin (BNS) possesses anti-serotonin 5-HT2A activity in addition to anti-dopamine D2 activity, which is characteristic of second-generation antipsychotics, little information is available on its pharmacologic profile in vivo. We investigated the BNS daily dose, plasma concentration, plasma anti-D2 activity, and plasma anti-5-HT2A activity in schizophrenia in a total of 14 subjects. Methods Blood samples were taken 14 days after the BNS dose was fixed, and the plasma concentration was measured by means of high-performance liquid chromatographic (HPLC) method. In addition, the plasma anti-D2 activity and anti-5-HT2A activity were measured by means of radioreceptor assays in which [3H]-spiperone and [3H]-ketanserin were used. Results The results revealed a statistically significant correlation between the daily dose and the plasma concentration (p = 0.04). Statistically significant correlations were also observed between the plasma concentration and the anti-D2 activity and between the plasma concentration and the anti-5-HT2A activity (p = 0.003 and 0.04). Conclusions It is therefore believed that both the anti-D2 activity in plasma and the anti-5-HT2A activity in plasma are regulated almost solely by the unchanged principal. Moreover, the mean plasma serotonin/dopamine (S/D) ratio was 0.9 and BNS exhibited both anti-D2 activity and also anti-5-HT2A activity in vivo, as well, so it was clear that the in vitro pharmacological profile was retained in vivo. |
| Author | Suzuki, Hidenobu Gen, Keishi |
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| References | Laszy J, Laszlovszky I, Gyertyan I. 2005. Dopamine D3 receptor antagonists improve the learning performance in memory impaired rats. Psychopharmacology (Ber1) 179: 567-575. Ceulemans DLS, Gelders YG, Hoppenbrouwers M-LJA, Reintjens AJM, Janssen PAJ. 1985. Effect of serotonin antagonism in schizophrenia: a pilot study with setoperone. Psychopharmacology 85: 329-332. Murasaki M, Nishikawa H, Ishibashi T. 2008. Dopamine-serotonin antagonist: receptor binding profile of a novel antipsychotic blonanserin. Jpn J Clin Phychopharmacol 11: 845-854. Carlsson A, Lindqvist M. 1963. Effects of chlorpromazine or haloperidol on formation of 3-methoxytyramine and normetanephrine in mouse brain. Acta Pharmacol Toxicol 20: 140-144. Kane J, Honigfeld G, Singer J, Meltzer H. 1988. Clozapine for the treatment-resistant schizophrenic: a double-blind comparison with chlorpromazine. Arch Gen Psychiatry 45: 489-796. Millan MJ. 2000. Improving the treatment of schizophrenia: focus on serotonin (5-HT)1A receptors. J Pharmacol Exp Ther 295: 853-861. Aoba A, Karita N, Yamaguchi N, et al. 1983. Electric convulsive therapy (ECT) increases plasma and blood cell haloperidol neuroleptic activities. Life Sci 33: 1797-1803. Aoba A, Karita N, Yamaguchi N, et al. 1985. Absence age effect on plasma haloperidol neuroleptic levels in psychiatric patients. J Gerontol 40: 303-308. Schotte A, Janssen PFM, Gommeren W, et al. 1996. Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. Psychopharmacology (Ber1) 124: 57-73. Kurumiya S, Une T. 2008. The research road to blonanserin, a new antipsychotic, and its pharmacological profile. Jpn J Clin Phychopharmacol 11: 807-815. Une T, Kurumiya S. 2007. Pharmacological profile of blonanserin. Jpn J Clin Phychopharmacol 10: 1263-1272. Murasaki M. 2008. Preclinical and clinical features of blonanserin. Jpn J Clin Phychopharmacol 11: 855-868. Noda Y, Kurumiya S, Miura Y, Oka M. 1993. Comparative study of 2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocychoocta[b]pyridine (AD-5423) and haloperidol for their pharmacological activities related to antipsychotic efficacy and/or adverse side effects. J Pharmacol Exp Ther 265: 745-751. Hedlund PB, Sutcliffe JG. 2004. Functional, molecular and pharmacological advances in 5-HT7 receptor research. Trends Pharmacol Sci 25: 481-486. Gen K, Morokawa Y, Aoba A. 2002. A study of plasma dopamine (D2) and plasma serotonin (5-HT2A) activity of risperidone, zotepine, and chlorpromazine-Is chlorpromazine an atypical antipsychotics? Jpn J Clin Phychopharmacol 5: 211-219. Matsumoto K, Yasumoto K, Nakamura H, Terazawa Y. 2008. The effect of erythromycin on the pharmacokinetics and safety of blonanserin in healthy male Japanese. Jpn J Clin Phychopharmacol 11: 891-899. Murasaki M. 2007. Clinical evaluation of blonanserin for schizophrenia-a randomized controlled study comparing blonanserin with haloperidol. Jpn J Clin Phychopharmacol 10: 2059-2079. Miura S. 2008. Clinical evaluation of blonanserin for schizophrenia-a randomized controlled study comparing blonanserin with risperidone. Jpn J Clin Phychopharmacol 11: 297-314. Dai D, Tang J, Rose R. 2001. Identification of variants of CYP 3A4 and characterization of their abilities to metabolize testosterone and chlorpyrifos. J Pharmacol Exp Ther 299: 825-831. Castelao F, Ferreira L, Gelders YG, Heilen SLE. 1989. The efficacy of the D2 and 5-HT-2 antagonist risperidone (R64766) in the treatment of chronic psychosis: an open dose-finding study. Schizophrenia Res 2: 411-415. Ishigooka J. 2008. An overview of clinical trials of blonanserin, a new antipsychotic drug with dopamine D2 and serotonin 5-HT2A antagonism. Jpn J Clin Phychopharmacol 11: 817-833. Oka M, Noda Y, Ochi Y, et al. 1993. Pharmacological profile of AD-5423, a novel antipsychotic with both potent dopamine-D2 and serotonin-S2 antagonist properties. J Pharmacol Exp Ther 264: 158-165. Suzuki H, Morokawa Y, Aoba A. 2003. Correlation between the plasma anti-serotonin (5-HT2A) and the plasma anti-dopamine (D2) activities of six typical and novel antipsychotic drugs and the ratio of anti-5-HT2A activity to anti-D2 activity (S/D ratio) in plasma. Jpn J Clin Phychopharmacol 6: 1595-1605. 1989; 2 2001; 299 1963; 20 2005; 179 2002; 5 2004; 25 2003; 6 1988; 45 2000; 295 1985; 40 1985; 85 2008; 11 2007; 10 1996; 124 1993; 264 1983; 33 1993; 265 |
| References_xml | – reference: Schotte A, Janssen PFM, Gommeren W, et al. 1996. Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. Psychopharmacology (Ber1) 124: 57-73. – reference: Castelao F, Ferreira L, Gelders YG, Heilen SLE. 1989. The efficacy of the D2 and 5-HT-2 antagonist risperidone (R64766) in the treatment of chronic psychosis: an open dose-finding study. Schizophrenia Res 2: 411-415. – reference: Dai D, Tang J, Rose R. 2001. Identification of variants of CYP 3A4 and characterization of their abilities to metabolize testosterone and chlorpyrifos. J Pharmacol Exp Ther 299: 825-831. – reference: Gen K, Morokawa Y, Aoba A. 2002. A study of plasma dopamine (D2) and plasma serotonin (5-HT2A) activity of risperidone, zotepine, and chlorpromazine-Is chlorpromazine an atypical antipsychotics? Jpn J Clin Phychopharmacol 5: 211-219. – reference: Aoba A, Karita N, Yamaguchi N, et al. 1983. Electric convulsive therapy (ECT) increases plasma and blood cell haloperidol neuroleptic activities. Life Sci 33: 1797-1803. – reference: Murasaki M. 2007. Clinical evaluation of blonanserin for schizophrenia-a randomized controlled study comparing blonanserin with haloperidol. Jpn J Clin Phychopharmacol 10: 2059-2079. – reference: Suzuki H, Morokawa Y, Aoba A. 2003. Correlation between the plasma anti-serotonin (5-HT2A) and the plasma anti-dopamine (D2) activities of six typical and novel antipsychotic drugs and the ratio of anti-5-HT2A activity to anti-D2 activity (S/D ratio) in plasma. Jpn J Clin Phychopharmacol 6: 1595-1605. – reference: Ishigooka J. 2008. An overview of clinical trials of blonanserin, a new antipsychotic drug with dopamine D2 and serotonin 5-HT2A antagonism. Jpn J Clin Phychopharmacol 11: 817-833. – reference: Laszy J, Laszlovszky I, Gyertyan I. 2005. Dopamine D3 receptor antagonists improve the learning performance in memory impaired rats. Psychopharmacology (Ber1) 179: 567-575. – reference: Ceulemans DLS, Gelders YG, Hoppenbrouwers M-LJA, Reintjens AJM, Janssen PAJ. 1985. Effect of serotonin antagonism in schizophrenia: a pilot study with setoperone. Psychopharmacology 85: 329-332. – reference: Matsumoto K, Yasumoto K, Nakamura H, Terazawa Y. 2008. The effect of erythromycin on the pharmacokinetics and safety of blonanserin in healthy male Japanese. Jpn J Clin Phychopharmacol 11: 891-899. – reference: Millan MJ. 2000. Improving the treatment of schizophrenia: focus on serotonin (5-HT)1A receptors. J Pharmacol Exp Ther 295: 853-861. – reference: Miura S. 2008. Clinical evaluation of blonanserin for schizophrenia-a randomized controlled study comparing blonanserin with risperidone. Jpn J Clin Phychopharmacol 11: 297-314. – reference: Kane J, Honigfeld G, Singer J, Meltzer H. 1988. Clozapine for the treatment-resistant schizophrenic: a double-blind comparison with chlorpromazine. Arch Gen Psychiatry 45: 489-796. – reference: Une T, Kurumiya S. 2007. Pharmacological profile of blonanserin. Jpn J Clin Phychopharmacol 10: 1263-1272. – reference: Murasaki M, Nishikawa H, Ishibashi T. 2008. Dopamine-serotonin antagonist: receptor binding profile of a novel antipsychotic blonanserin. Jpn J Clin Phychopharmacol 11: 845-854. – reference: Hedlund PB, Sutcliffe JG. 2004. Functional, molecular and pharmacological advances in 5-HT7 receptor research. Trends Pharmacol Sci 25: 481-486. – reference: Noda Y, Kurumiya S, Miura Y, Oka M. 1993. Comparative study of 2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocychoocta[b]pyridine (AD-5423) and haloperidol for their pharmacological activities related to antipsychotic efficacy and/or adverse side effects. J Pharmacol Exp Ther 265: 745-751. – reference: Carlsson A, Lindqvist M. 1963. Effects of chlorpromazine or haloperidol on formation of 3-methoxytyramine and normetanephrine in mouse brain. 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Blonanserin (BNS) possesses anti‐serotonin 5‐HT2A activity in addition to anti‐dopamine D2 activity, which is characteristic of second‐generation... Blonanserin (BNS) possesses anti-serotonin 5-HT(2A) activity in addition to anti-dopamine D(2) activity, which is characteristic of second-generation... Objective Blonanserin (BNS) possesses anti-serotonin 5-HT2A activity in addition to anti-dopamine D2 activity, which is characteristic of second-generation... |
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| SubjectTerms | Adult Aged anti-dopamine D2 activity anti-serotonin 5-HT2A activity Antipsychotic Agents - administration & dosage Antipsychotic Agents - blood Azides - administration & dosage Azides - blood blonanserin Brain - drug effects Dopamine Antagonists - administration & dosage Dopamine Antagonists - blood Dopamine D2 Receptor Antagonists Female Humans Male Middle Aged Piperazines - administration & dosage Piperazines - blood Piperidines - administration & dosage Piperidines - blood plasma concentration Radioligand Assay radioreceptor assay Serotonin - administration & dosage Serotonin - analogs & derivatives Serotonin - blood Serotonin 5-HT2 Receptor Antagonists |
| Title | The relationship between the daily dose, the plasma concentration of blonanserin, and its plasma anti-dopamine D2 and anti-serotonin 5-HT2A activity |
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