Blonanserin: Difference between revisions

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{{Drugbox
{{Drugbox
| IUPAC_name = 2-(4-ethylpiperazin-1-yl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine
| IUPAC_name = 2-(4-ethylpiperazin-1-yl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine
| image = Blonanserin.png
| image = Blonanserin.png
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| InChI = 1/C23H30FN3/c1-2-26-13-15-27(16-14-26)23-17-21(18-9-11-19(24)12-10-18)20-7-5-3-4-6-8-22(20)25-23/h9-12,17H,2-8,13-16H2,1H3
| ChemSpiderID = 111697
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| InChIKey = XVGOZDAJGBALKS-UHFFFAOYAW
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| InChI = 1/C23H30FN3/c1-2-26-13-15-27(16-14-26)23-17-21(18-9-11-19(24)12-10-18)20-7-5-3-4-6-8-22(20)25-23/h9-12,17H,2-8,13-16H2,1H3
| CAS_number = 132810-10-7
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| InChIKey = XVGOZDAJGBALKS-UHFFFAOYAW
| CAS_number = 132810-10-7
| ATC_prefix = none
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| ATC_suffix =
| CAS_supplemental =
| ATC_prefix = none
| PubChem = 125564
| ATC_suffix =
| ChemSpiderID = 111697
| C = 23 | H = 30 | F = 1 | N = 3
| ATC_supplemental =
| PubChem = 125564
| molecular_weight = 367.50 g/mol
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| smiles = Fc1ccc(cc1)c2cc(nc3c2CCCCCC3)N4CCN(CC)CC4
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| DrugBank =
| chemical_formula =
| bioavailability =
| C=23 | H=30 | F=1 | N=3
| metabolism =
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| elimination_half-life =
| molecular_weight = 367.50 g/mol
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| excretion =
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| smiles = Fc1ccc(cc1)c2cc(nc3c2CCCCCC3)N4CCN(CC)CC4
| bioavailability =
| pregnancy_category =
| protein_bound =
| legal_status = Rx-only
| metabolism =
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| elimination_half-life =
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| excretion =
| pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X -->
| pregnancy_US = <!-- A / B / C / D / X -->
| pregnancy_category=
| legal_AU = <!-- S2, S3, S4, S5, S6, S7, S8, S9 or Unscheduled-->
| legal_CA = <!-- Schedule I, II, III, IV, V, VI, VII, VIII -->
| legal_UK = <!-- GSL, P, POM, CD, or Class A, B, C -->
| legal_US = <!-- OTC / Rx-only / Schedule I, II, III, IV, V -->
| legal_status = Rx-only
| routes_of_administration = Oral
| routes_of_administration = Oral
}}
}}


'''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> Blonanserin 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]] (K<sub>i</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> It lacks significant [[affinity (pharmacology)|affinity]] for numerous other sites including [[D1 receptor|D<sub>1</sub>]], [[5-HT3 receptor|5-HT<sub>3</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''' ([[International Nonproprietary Name|INN]], also known as '''AD-5423''' and marketed under the brand name '''Lonasen''') is a [[5-HT receptor|5-HT<sub>2</sub> receptor]] [[Receptor antagonist|antagonist]] and [[Dopamine receptor D2|Dopamine receptor D<sub>2</sub>]] antagonist<ref>Oka M, Noda Y, Ochi Y, Furukawa K, Une T, Kurumiya S, Hino K, Karasawa T. Pharmacological profile of AD-5423, a novel antipsychotic with both potent dopamine-D2 and serotonin-S2 antagonist properties. ''Journal of Pharmacology and Experimental Therapeutics''. 1993 Jan;264(1):158-65. PMID 8093723</ref> used as an [[antipsychotic]].<ref>Ochi T, Sakamoto M, Minamida A, Suzuki K, Ueda T, Une T, Toda H, Matsumoto K, Terauchi Y. Syntheses and properties of the major hydroxy metabolites in humans of blonanserin AD-5423, a novel antipsychotic agent. ''Bioorganic and Medicinal Chemistry Letters''. 2005 Feb 15;15(4):1055-9. PMID 15686911</ref>


== See also ==
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{{pharma-stub}}
* [[Atypical antipsychotic]]

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== References ==
{{Reflist|2}}


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==References==
{{reflist}}


{{Antipsychotics}}
{{Antipsychotics}}
{{Serotonergics}}
{{Adrenergics}}
{{Dopaminergics}}
{{Dopaminergics}}
{{Serotonergics}}
{{Piperazines}}


[[Category:Antipsychotics]]
[[Category:Antipsychotics]]
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[[Category:Dopamine antagonists]]
[[Category:Dopamine antagonists]]
[[ja:ブロナンセリン]]
[[ja:ブロナンセリン]]


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{{pharmacology-stub}}

Revision as of 00:51, 10 March 2010

Blonanserin
Clinical data
Routes of
administration		Oral
ATC code
  • none
Legal status
Legal status
  • In general: ℞ (Prescription only)
Identifiers
  • 2-(4-ethylpiperazin-1-yl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine
CAS Number
PubChem CID
ChemSpider
CompTox Dashboard (EPA)
ECHA InfoCard100.211.656 Edit this at Wikidata
Chemical and physical data
FormulaC23H30FN3
Molar mass367.50 g/mol g·mol−1
3D model (JSmol)
  • Fc1ccc(cc1)c2cc(nc3c2CCCCCC3)N4CCN(CC)CC4

Blonanserin (Lonasen) is a relatively new atypical antipsychotic commercialized by Dainippon Sumitomo Pharma in Japan and Korea for the treatment of schizophrenia.[1] It acts as a mixed 5-HT2 (Ki = 3.98 nM) and D2 receptor (Ki = 14.8 nM) antagonist.[2] Blonanserin also exerts some blockade of α1-adrenergic receptors (Ki = 56.3 nM) and has low affinity for the sigma receptor (Ki = 286 nM).[2] It lacks significant affinity for numerous other sites including D1, 5-HT3, α2-adrenergic, β-adrenergic, H1, mACh, and the monoamine transporters.

See also

References

  1. ^ 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)
  2. ^ 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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