Blonanserin
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Blonanserin
structure -
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CAS No:
132810-10-7
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Formula:
C23H30FN3
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Chemical Name:
Blonanserin
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Synonyms:
Cycloocta[b]pyridine,2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydro-;2-(4-Ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine;AD 5423;Blonanserin;Lonasen
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CAS No:
Description
Pale Yellow SolidBlonanserin, a dual antagonist of dopamine D2 and serotonin 5-HT2 receptors, was launched past year in Japan for the oral treatment of psychosis and schizophrenia. It is the latest entry in the class of atypical antipsychotic agents to reach the market. Blonanserin exhibits high affinity for D2 and 5-HT2 receptors (IC50 23.6 and 9.85 nM, respectively). Its affinity for D2 receptors is very close to that of haloperidol and risperidone, whereas the affinity for 5-HT2 receptors i
Blonanserin is an organic molecular entity.|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.
Characteristics
19.4
5.266
white to off-white
1.095±0.06 g/cm3(Predicted)
117-119°C
540.8±50.0 °C(Predicted)
280.9±30.1 °C
1.557
DMSO: ≥10mg/mL
Refrigerator
9.21E-12mmHg at 25°C
Safety Information
NONH for all modes of transport
1
22
GY0175140
Xn
P264, P270, P273, P301+P312, P330, P501
H302-H413
|Warning|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|P264, P270, P273, P301+P312, P330, and P501|Aggregated GHS information provided by 40 companies from 2 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.
Toxicity
Oral LD50 of >500 mg/kg in mice.
Blonanserin is over 99.7% bound to plasma proteins . Serum albumin is the primary binder.
Drug Information
Used for the treatment of schizophrenia.
Blonanserin antagonizes dopamine and serotonin receptors to reduce symptoms of schizophrenia.
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.|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.|Blonanserin has a Vc of 9500 L and a Vt of 8560 L for a total Vd of 18060 L.|Blonanserin has a clearance of 1230 L/h.
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.
Blonanserin has a half life of elimination of 10.7-16.2 h.
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.
2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta(b)pyridine
Blonanserin Use and Manufacturing
A 5-HT2 Serotonin receptor and D2 Dopamine receptor antagonist, used as an antipsychotic.
Computed Properties
Molecular Weight:367.5
XLogP3:5.5
Hydrogen Bond Acceptor Count:4
Rotatable Bond Count:3
Exact Mass:367.24237613
Monoisotopic Mass:367.24237613
Topological Polar Surface Area:19.4
Heavy Atom Count:27
Complexity:443
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes
Registered Holders
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Marubeni Pharmaceuticals (Suzhou) Co., Ltd.
Active
China
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Biobetta Pharmaceuticals (Shanghai) Co., Ltd.
Active
China
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Hebei Anjian Chengyi Pharmaceutical Technology Co., Ltd.
Active
China
Recommended Suppliers of Blonanserin
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Business licensedTrader Supplier of Avibactam Sodium,Blonanserin,Relebactam,TofacitinibBlonanserin; 2-(4-Ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridineInquiryCAS No.: 132810-10-7Grade: Pharmaceutical GradeContent: 99% -
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