| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Purity: ≥98%
Blonanserin (formerly AD 5423; AD-5423; AD5423) is an atypical antipsychotic agent acting as a relatively selective serotonin (5-HT)2A and dopamine D2 antagonist with the potential to be used for the treatment of schizophrenia. Blonanserin has a better tolerability profile than many other antipsychotics because it doesn't cause side effects like hypotension, excessive sedation, or extrapyramidal symptoms. Blonanserin, like many other 2nd-generation (atypical) antipsychotics, is much more effective than haloperidol or other 1st-generation (typical) antipsychotics at treating the negative symptoms of schizophrenia.
| Targets |
D2 Receptor ( Ki = 0.142 nM ); D3 Receptor ( Ki = 0.494 nM ); D4 Receptor ( Ki = 150 nM ); D1 Receptor ( Ki = 1070 nM ); 5-HT2A Receptor ( Ki = 0.812 nM );
5-HT2C Receptor ( Ki = 26.4 nM ); 5-HT6 Receptor ( Ki = 11.7 nM ); α1-adrenergic receptor ( Ki = 26.7 ); α2-adrenergic receptor ( Ki = 530 ) |
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| ln Vitro |
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| ln Vivo |
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| Animal Protocol |
Mice received saline or phencyclidine once a day for 14 consecutive days
1 mg/kg Oral gavage; 1 mg/kg; 14 days |
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
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. 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. Biological Half-Life Blonanserin has a half life of elimination of 10.7-16.2 h. |
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| Toxicity/Toxicokinetics |
Protein Binding
Blonanserin is over 99.7% bound to plasma proteins . Serum albumin is the primary binder. |
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| References | ||
| Additional Infomation |
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. Drug Indication Used for the treatment of schizophrenia. 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. |
| Molecular Formula |
C23H30FN3
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| Molecular Weight |
367.5
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| Exact Mass |
367.242
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| Elemental Analysis |
C, 75.17; H, 8.23; F, 5.17; N, 11.43
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| CAS # |
132810-10-7
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| Related CAS # |
Blonanserin-d5; 1346599-86-7; Blonanserin dihydrochloride; 132812-45-4; Blonanserin-d8; 132812-47-6 (citrate)
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| PubChem CID |
125564
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| Appearance |
Solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
540.8±50.0 °C at 760 mmHg
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| Melting Point |
117-119°C
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| Flash Point |
280.9±30.1 °C
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| Vapour Pressure |
0.0±1.4 mmHg at 25°C
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| Index of Refraction |
1.557
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| LogP |
6.03
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
27
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| Complexity |
443
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1C([H])=C([H])C(=C([H])C=1[H])C1=C([H])C(=NC2C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C=21)N1C([H])([H])C([H])([H])N(C([H])([H])C([H])([H])[H])C([H])([H])C1([H])[H]
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| InChi Key |
XVGOZDAJGBALKS-UHFFFAOYSA-N
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| InChi Code |
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
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| Chemical Name |
2-(4-ethylpiperazin-1-yl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.43 mg/mL (3.89 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 14.3 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.43 mg/mL (3.89 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 14.3 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.43 mg/mL (3.89 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7211 mL | 13.6054 mL | 27.2109 mL | |
| 5 mM | 0.5442 mL | 2.7211 mL | 5.4422 mL | |
| 10 mM | 0.2721 mL | 1.3605 mL | 2.7211 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01796730 | Completed | Drug: bambuterol Drug: Placebo |
COPD | The First Affiliated Hospital of Guangzhou Medical University |
February 2013 | Phase 4 |
Products are for research use only; We do not sell to patients
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