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Purity: ≥98%
Bavisant (also known as JNJ-31001074) is a novel, highly selective, orally bioactive antagonist of the human H3 receptor with a novel mechanism of action which involves wakefulness and cognition. It could be applied as an ADHD treatment. H3 antagonists may help with impulsivity and attention since histamine H3 receptors are found on non-histamine neurons and control other neurotransmitters like acetylcholine and norepinephrine. Research suggests that H3 receptor antagonists may have a special therapeutic effect and provide a significant alternative for the treatment of ADHD because of their novel mechanism of action.
| Targets |
H3 receptor
|
|---|---|
| ln Vitro |
Bavisant raises acetylcholine levels in rat frontal cortex[4].
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| ln Vivo |
Bavisant increases acetylcholine levels in the frontal cortex of rats [4].
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| References |
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| Molecular Formula |
C19H27N3O2
|
|---|---|
| Molecular Weight |
329.43658
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| Exact Mass |
329.21
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| Elemental Analysis |
C, 69.27; H, 8.26; N, 12.76; O, 9.71
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| CAS # |
929622-08-2
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| Related CAS # |
Bavisant dihydrochloride hydrate; 1103522-80-0; Bavisant dihydrochloride; 929622-09-3
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| Appearance |
Solid powder
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| SMILES |
C1CC1N2CCN(CC2)C(=O)C3=CC=C(C=C3)CN4CCOCC4
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| InChi Key |
BGBVSGSIXIIREO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H27N3O2/c23-19(22-9-7-21(8-10-22)18-5-6-18)17-3-1-16(2-4-17)15-20-11-13-24-14-12-20/h1-4,18H,5-15H2
|
| Chemical Name |
(4-cyclopropylpiperazin-1-yl)-[4-(morpholin-4-ylmethyl)phenyl]methanone
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| Synonyms |
JNJ-31001074; JNJ31001074; JNJ 31001074; Bavisant dihydrochloride
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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 |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~303.6 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.59 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 25.0 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: ≥ 2.5 mg/mL (7.59 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 25.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0355 mL | 15.1773 mL | 30.3545 mL | |
| 5 mM | 0.6071 mL | 3.0355 mL | 6.0709 mL | |
| 10 mM | 0.3035 mL | 1.5177 mL | 3.0355 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 |
| NCT00915434 | Completed | Drug: JNJ-31001074 | Healthy Pharmacokinetics |
Johnson & Johnson Pharmaceutical Research & Development, L.L.C. |
June 2009 | Phase 1 |
| NCT00915746 | Completed | Drug: JNJ-31001074; ketoconazole | Healthy Pharmacokinetics Drug Interactions |
Johnson & Johnson Pharmaceutical Research & Development, L.L.C. |
November 2009 | Phase 1 |
| NCT00566449 | Completed | Drug: Placebo Drug: JNJ-31001074 |
Attention Deficit Hyperactivity Disorder |
Johnson & Johnson Pharmaceutical Research & Development, L.L.C. |
December 2007 | Phase 2 |
| NCT00566449 | Completed | Drug: Placebo Drug: JNJ-31001074 |
Attention Deficit Hyperactivity Disorder |
Johnson & Johnson Pharmaceutical Research & Development, L.L.C. |
December 2007 | Phase 2 |
| NCT00890240 | Completed | Drug: JNJ-31001074 | Attention Deficit Hyperactivity Disorder Attention Deficit Disorders With Hyperactivity |
Johnson & Johnson Pharmaceutical Research & Development, L.L.C. |
May 2009 | Phase 1 |
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