| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
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| ln Vivo |
The oral drug osanetant (SR142801; 1–10 mg/kg; taken 60 minutes prior to testing) dramatically lengthens the duration of social interactions [1]. Immobility time is shortened by oasanetant (ip; 5 and 10 mg/kg; 30 minutes prior to testing) [1].
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| Animal Protocol |
Animal/Disease Models: 7weeks old male gerbil (50-60 g) [1]
Doses: 1, 3 and 10 mg/kg Route of Administration: Po; 60 minutes before testing Experimental Results: Significant increase in social interaction time. |
| References | |
| Additional Infomation |
Developed by Sanofi-Aventis (formerly Sanofi-Synthelabo), osanetant (SR-142801) is an NK3 receptor antagonist which was under development for the treatment of schizophrenia and other Central Nervous System (CNS) disorders. In a review of its R&D portfolio, the company announced in August 2005 that it would cease any further development of osanetant. This follows an earlier decision to discontinue development of eplivanserin for schizophrenia.
Osanetant is an orally bioavailable, brain penetrating, non-peptide neurokinin/tachykinin 3 receptor (NK1-receptor; NK3R; NK-3R) antagonist, that may potentially be used to treat vasomotor symptoms (VMS) in menopausal woman and in men on androgen deprivation therapy (ADT) and to suppress the production of certain hormones. Upon oral administration, osanetant targets, competitively binds to and blocks the activity of NK3R in the central nervous system (CNS), thereby inhibiting NK3R-mediated signal transduction and may prevent certain menopausal symptoms such as hot flashes and VMS in men deprived of androgen. Neurokinin-mediated signaling may increase during hormone deficiency and may cause hot flashes. In addition, osanetant may, by inhibiting NK3R, suppress secretion of various hormones, such as testosterone, luteinizing hormone (LH) and follicle-stimulating hormone (FSH). By suppressing testosterone production, osanetant may inhibit the proliferation of hormone-sensitive prostate cancer. Drug Indication Potential therapy for schizophrenia, depression and visceral pain. Mechanism of Action The mechanism of action of osanetant is uncertain at this point. Various preclinical data indicate that activation of NK3 receptors enhances the release of biogenic amines, including dopamine and serotonin. NK3 receptor antagonists could block NK3-receptor-mediated activation of these systems. Pharmacodynamics Osanetant is a neurokinin-3 (NK3) receptor antagonist. Preliminary clinical trials have demonstrated that osanetant is superior to placebo on global assessment of efficacy and measures of positive symptoms in schizophrenia. |
| Molecular Formula |
C35H41CL2N3O2
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|---|---|
| Molecular Weight |
606.63
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| Exact Mass |
605.258
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| CAS # |
160492-56-8
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| Related CAS # |
(S)-Osanetant;182621-58-5
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| PubChem CID |
219077
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| Appearance |
White to off-white solid powder
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| Density |
1.25g/cm3
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| Boiling Point |
727.9ºC at 760mmHg
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| Flash Point |
394ºC
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| Vapour Pressure |
4.79E-21mmHg at 25°C
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| Index of Refraction |
1.633
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| LogP |
7.293
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
42
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| Complexity |
897
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC(=O)N(C)C1(CCN(CC1)CCC[C@@]2(CCCN(C2)C(=O)C3=CC=CC=C3)C4=CC(=C(C=C4)Cl)Cl)C5=CC=CC=C5
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| InChi Key |
DZOJBGLFWINFBF-UMSFTDKQSA-N
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| InChi Code |
InChI=1S/C35H41Cl2N3O2/c1-27(41)38(2)35(29-13-7-4-8-14-29)19-23-39(24-20-35)21-9-17-34(30-15-16-31(36)32(37)25-30)18-10-22-40(26-34)33(42)28-11-5-3-6-12-28/h3-8,11-16,25H,9-10,17-24,26H2,1-2H3/t34-/m0/s1
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| Chemical Name |
N-[1-[3-[(3R)-1-benzoyl-3-(3,4-dichlorophenyl)piperidin-3-yl]propyl]-4-phenylpiperidin-4-yl]-N-methylacetamide
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| Synonyms |
SR 142801; SR142801; SR-142801
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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)
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| Solubility (In Vitro) |
DMSO : ~66.67 mg/mL (~109.90 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.12 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 (4.12 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6485 mL | 8.2423 mL | 16.4845 mL | |
| 5 mM | 0.3297 mL | 1.6485 mL | 3.2969 mL | |
| 10 mM | 0.1648 mL | 0.8242 mL | 1.6485 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.
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