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    Blonanserin

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    2D Structure
    Also known as: 132810-10-7, Lonasen, Ad-5423, Blonanserin [inn], Ad 5423, 2-(4-ethylpiperazin-1-yl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine
    Molecular Formula
    C23H30FN3
    Molecular Weight
    367.5  g/mol
    InChI Key
    XVGOZDAJGBALKS-UHFFFAOYSA-N
    FDA UNII
    AQ316B4F8C
    Blonanserin is an atypical antipsychotic approved in Japan in January, 2008. It offers improved tolerability as it lacks side effects such as extrapyramidal symptoms, excessive sedation, or hypotension. As a second-generation (atypical) antipsychotic, it is significantly more efficacious in the treatment of the negative symptoms of schizophrenia compared to first-generation (typical) antipsychotics.
    1 2D Structure

    2D Structure

    2 Identification
    2.1 Computed Descriptors
    2.1.1 IUPAC Name
    2-(4-ethylpiperazin-1-yl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine
    2.1.2 InChI
    InChI=1S/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
    2.1.3 InChI Key
    XVGOZDAJGBALKS-UHFFFAOYSA-N
    2.1.4 Canonical SMILES
    CCN1CCN(CC1)C2=NC3=C(CCCCCC3)C(=C2)C4=CC=C(C=C4)F
    2.2 Other Identifiers
    2.2.1 UNII
    AQ316B4F8C
    2.3 Synonyms
    2.3.1 MeSH Synonyms

    1. 2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta(b)pyridine

    2. Ad 5423

    3. Ad-5423

    4. Ad5423

    5. Cycloocta(b)pyridine, 2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydro-

    6. Lonasen

    2.3.2 Depositor-Supplied Synonyms

    1. 132810-10-7

    2. Lonasen

    3. Ad-5423

    4. Blonanserin [inn]

    5. Ad 5423

    6. 2-(4-ethylpiperazin-1-yl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine

    7. Blonanserin (lonasen)

    8. 2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta(b)pyridine

    9. Aq316b4f8c

    10. Chembl178803

    11. 132810-10-7 (free Base)

    12. 2-(4-ethyl-1-piperazinyl)-4-(p-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta(b)pyridine

    13. Ncgc00183858-01

    14. 2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine

    15. Cycloocta(b)pyridine, 2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydro-

    16. 2-(4-ethylpiperazin-1-yl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine.

    17. Blonanserin (jan/inn)

    18. Unii-aq316b4f8c

    19. 2-(4-ethylpiperazin-1-yl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta(b)pyridine

    20. Cycloocta[b]pyridine, 2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydro-

    21. Ad5423

    22. Blonanserin [mi]

    23. Blonanserin [jan]

    24. Blonanserin(ad-5423)

    25. Blonanserin [mart.]

    26. Dsstox_cid_28716

    27. Dsstox_rid_82985

    28. Dsstox_gsid_48790

    29. Blonanserin [who-dd]

    30. Schembl119669

    31. Gtpl7670

    32. Dtxsid7048790

    33. Blonanserin, >=98% (hplc)

    34. Chebi:31296

    35. Amy8830

    36. Ex-a663

    37. Hms3740e13

    38. Zinc597434

    39. Bcp04236

    40. Dsp-5423

    41. Tox21_113267

    42. Bdbm50160807

    43. Mfcd00893838

    44. Pdsp1_000720

    45. Pdsp2_000710

    46. S2112

    47. Akos005145823

    48. Ac-1599

    49. Db09223

    50. Sb17396

    51. Cycloocta(b)pyridine, 2-(4-ethyl-1-piperazinyl)-4-(1-fluorophenyl)-5,6,7,8,9,10-hexahydro-

    52. As-11421

    53. Hy-13575

    54. A8384

    55. B4565

    56. Cas-132810-10-7

    57. Ft-0663415

    58. Ad-5423;ad5423;ad 5423

    59. D01176

    60. Ab01565798_02

    61. 810b107

    62. L001392

    63. Sr-01000945256

    64. Q4927426

    65. Sr-01000945256-1

    66. 4-(4-fluoro-phenyl)-2-(4-propyl-piperazin-1-yl)-5,6,7,8,9,10-hexahydro-cycloocta[b]pyridine

    2.4 Create Date
    2005-06-24
    3 Chemical and Physical Properties
    Molecular Weight 367.5 g/mol
    Molecular Formula C23H30FN3
    XLogP35.5
    Hydrogen Bond Donor Count0
    Hydrogen Bond Acceptor Count4
    Rotatable Bond Count3
    Exact Mass367.24237613 g/mol
    Monoisotopic Mass367.24237613 g/mol
    Topological Polar Surface Area19.4 Ų
    Heavy Atom Count27
    Formal Charge0
    Complexity443
    Isotope Atom Count0
    Defined Atom Stereocenter Count0
    Undefined Atom Stereocenter Count0
    Defined Bond Stereocenter Count0
    Undefined Bond Stereocenter Count0
    Covalently Bonded Unit Count1
    4 Drug and Medication Information
    4.1 Drug Indication

    Used for the treatment of schizophrenia.

    5 Pharmacology and Biochemistry
    5.1 Pharmacology

    Blonanserin antagonizes dopamine and serotonin receptors to reduce symptoms of schizophrenia.

    5.2 Absorption, Distribution and Excretion

    Absorption

    Blonanserin has a Tmax of 1.5 h and a bioavailablity of 55%. Tmax has been observed to be prolonged and relative bioavailability increased when administered with food.

    Route of Elimination

    57% of blonanserin is excreted in the urine and 30% in the feces. Only 5% of the drug in the feces is the parent drug with no parent drug excreted through the urine.

    Volume of Distribution

    Blonanserin has a Vc of 9500 L and a Vt of 8560 L for a total Vd of 18060 L.

    Clearance

    Blonanserin has a clearance of 1230 L/h.

    5.3 Metabolism/Metabolites

    Blonanserin is mainly metabolized by CYP3A4. It undergoes hydoxylation of the cyclooctane ring as well as N-oxidation and N-deethylation of the piperazine ring. The N-deethylated and hydroxylated metabolites are active but to a lesser degree than the parent drug.

    5.4 Biological Half-Life

    Blonanserin has a half life of elimination of 10.7-16.2 h.

    5.5 Mechanism of Action

    Blonanserin binds to and inhibits dopamine receptors D2 and D3 as well as the serotonin receptor 5-HT2A with high affinity. Blonanserin has low affinity for other dopamine and serotonin receptors as well as muscarinic, adrenergic, and histamine receptors. This reduces dopaminergic and serotonergic neurotransmission which is thought to produce a reduction in positive and negative symptoms of schizophrenia respectively.