Blonanserin: Difference between revisions
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'''Blonanserin''' ('''Lonasen''') is a relatively new [[atypical antipsychotic]] commercialized by [[Dainippon Sumitomo Pharma]] in [[Japan]] and [[Korea]] for the treatment of [[schizophrenia]].<ref name="pmid20030420">{{cite journal | author = Deeks ED, Keating GM | title = Blonanserin: a review of its use in the management of schizophrenia | journal = CNS Drugs | volume = 24 | issue = 1 | pages = 65–84 | year = 2010 | month = January | pmid = 20030420 | doi = 10.2165/11202620-000000000-00000 | url = http://content.wkhealth.com/linkback/openurl?issn=1172-7047&volume=24&issue=1&spage=65}}</ref> It acts as a mixed [[5-HT2 receptor|5-HT<sub>2</sub>]] (K<sub>i</sub> = 3.98 nM) and [[D2 receptor|D<sub>2</sub> receptor]] (K<sub>i</sub> = 14.8 nM) [[receptor antagonist|antagonist]].<ref name="pmid8093723">{{cite journal | author = Oka M, Noda Y, Ochi Y, ''et al.'' | title = Pharmacological profile of AD-5423, a novel antipsychotic with both potent dopamine-D2 and serotonin-S2 antagonist properties | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 264 | issue = 1 | pages = 158–65 | year = 1993 | month = January | pmid = 8093723 | doi = | url = http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=8093723}}</ref> It also exerts some blockade of [[alpha-1 adrenergic receptor|α<sub>1</sub>-adrenergic receptor]]s (K<sub>i</sub> = 56.3 nM) and has low [[affinity (pharmacology)|affinity]] for the [[sigma receptor]] (IC<sub>50</sub> = 286 nM).<ref name="pmid8093723">{{cite journal | author = Oka M, Noda Y, Ochi Y, ''et al.'' | title = Pharmacological profile of AD-5423, a novel antipsychotic with both potent dopamine-D2 and serotonin-S2 antagonist properties | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 264 | issue = 1 | pages = 158–65 | year = 1993 | month = January | pmid = 8093723 | doi = | url = http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=8093723}}</ref> Blonanserin lacks significant affinity for numerous other sites including [[5-HT1 receptor|5-HT<sub>1</sub>]], [[5-HT3 receptor|5-HT<sub>3</sub>]], [[D1 receptor|D<sub>1</sub>]], [[alpha-2 adrenergic receptor|α<sub>2</sub>-adrenergic]], [[beta-adrenergic receptor|β-adrenergic]], [[H1 receptor|H<sub>1</sub>]], [[muscarinic acetylcholine receptor|mACh]], and the [[monoamine transporter]]s. |
'''Blonanserin''' ('''Lonasen''') is a relatively new [[atypical antipsychotic]] commercialized by [[Dainippon Sumitomo Pharma]] in [[Japan]] and [[Korea]] for the treatment of [[schizophrenia]].<ref name="pmid20030420">{{cite journal | author = Deeks ED, Keating GM | title = Blonanserin: a review of its use in the management of schizophrenia | journal = CNS Drugs | volume = 24 | issue = 1 | pages = 65–84 | year = 2010 | month = January | pmid = 20030420 | doi = 10.2165/11202620-000000000-00000 | url = http://content.wkhealth.com/linkback/openurl?issn=1172-7047&volume=24&issue=1&spage=65}}</ref><ref name="pmid19552488">{{cite journal | author = Garcia E, Robert M, Peris F, Nakamura H, Sato N, Terazawa Y | title = The efficacy and safety of blonanserin compared with haloperidol in acute-phase schizophrenia: a randomized, double-blind, placebo-controlled, multicentre study | journal = CNS Drugs | volume = 23 | issue = 7 | pages = 615–25 | year = 2009 | pmid = 19552488 | doi = | url = http://content.wkhealth.com/linkback/openurl?issn=1172-7047&volume=23&issue=7&spage=615}}</ref><ref name="pmid18465651">{{cite journal | author = Heading CE | title = AD-5423 (Dainippon Pharmaceutical Co Ltd) | journal = IDrugs : the Investigational Drugs Journal | volume = 1 | issue = 7 | pages = 813–7 | year = 1998 | month = November | pmid = 18465651 | doi = | url = }}</ref> It acts as a mixed [[5-HT2 receptor|5-HT<sub>2</sub>]] (K<sub>i</sub> = 3.98 nM) and [[D2 receptor|D<sub>2</sub> receptor]] (K<sub>i</sub> = 14.8 nM) [[receptor antagonist|antagonist]].<ref name="pmid8093723">{{cite journal | author = Oka M, Noda Y, Ochi Y, ''et al.'' | title = Pharmacological profile of AD-5423, a novel antipsychotic with both potent dopamine-D2 and serotonin-S2 antagonist properties | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 264 | issue = 1 | pages = 158–65 | year = 1993 | month = January | pmid = 8093723 | doi = | url = http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=8093723}}</ref> It also exerts some blockade of [[alpha-1 adrenergic receptor|α<sub>1</sub>-adrenergic receptor]]s (K<sub>i</sub> = 56.3 nM) and has low [[affinity (pharmacology)|affinity]] for the [[sigma receptor]] (IC<sub>50</sub> = 286 nM).<ref name="pmid8093723">{{cite journal | author = Oka M, Noda Y, Ochi Y, ''et al.'' | title = Pharmacological profile of AD-5423, a novel antipsychotic with both potent dopamine-D2 and serotonin-S2 antagonist properties | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 264 | issue = 1 | pages = 158–65 | year = 1993 | month = January | pmid = 8093723 | doi = | url = http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=8093723}}</ref> Blonanserin lacks significant affinity for numerous other sites including [[5-HT1 receptor|5-HT<sub>1</sub>]], [[5-HT3 receptor|5-HT<sub>3</sub>]], [[D1 receptor|D<sub>1</sub>]], [[alpha-2 adrenergic receptor|α<sub>2</sub>-adrenergic]], [[beta-adrenergic receptor|β-adrenergic]], [[H1 receptor|H<sub>1</sub>]], [[muscarinic acetylcholine receptor|mACh]], and the [[monoamine transporter]]s. |
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== See also == |
== See also == |
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Revision as of 00:58, 10 March 2010
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| Routes of administration | Oral |
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| CompTox Dashboard (EPA) | |
| ECHA InfoCard | 100.211.656 |
| Chemical and physical data | |
| Formula | C23H30FN3 |
| Molar mass | 367.50 g/mol g·mol−1 |
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Blonanserin (Lonasen) is a relatively new atypical antipsychotic commercialized by Dainippon Sumitomo Pharma in Japan and Korea for the treatment of schizophrenia.[1][2][3] It acts as a mixed 5-HT2 (Ki = 3.98 nM) and D2 receptor (Ki = 14.8 nM) antagonist.[4] It also exerts some blockade of α1-adrenergic receptors (Ki = 56.3 nM) and has low affinity for the sigma receptor (IC50 = 286 nM).[4] Blonanserin lacks significant affinity for numerous other sites including 5-HT1, 5-HT3, D1, α2-adrenergic, β-adrenergic, H1, mACh, and the monoamine transporters.
See also
References
- ^ Deeks ED, Keating GM (2010). "Blonanserin: a review of its use in the management of schizophrenia". CNS Drugs. 24 (1): 65–84. doi:10.2165/11202620-000000000-00000. PMID 20030420.
{{cite journal}}: Unknown parameter|month=ignored (help) - ^ Garcia E, Robert M, Peris F, Nakamura H, Sato N, Terazawa Y (2009). "The efficacy and safety of blonanserin compared with haloperidol in acute-phase schizophrenia: a randomized, double-blind, placebo-controlled, multicentre study". CNS Drugs. 23 (7): 615–25. PMID 19552488.
{{cite journal}}: CS1 maint: multiple names: authors list (link) - ^ Heading CE (1998). "AD-5423 (Dainippon Pharmaceutical Co Ltd)". IDrugs : the Investigational Drugs Journal. 1 (7): 813–7. PMID 18465651.
{{cite journal}}: Unknown parameter|month=ignored (help) - ^ a b 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". The Journal of Pharmacology and Experimental Therapeutics. 264 (1): 158–65. PMID 8093723.
{{cite journal}}: Explicit use of et al. in:|author=(help); Unknown parameter|month=ignored (help)CS1 maint: multiple names: authors list (link)
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