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].

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.

[1]. Selective blockade of NK2 or NK3 receptors produces anxiolytic- and antidepressant-like effects in gerbils. Pharmacol Biochem Behav. 2006 Apr;83(4):533-9.

Oxanetainetan (SR-142801), developed by Sanofi-Aventis (formerly Sanofi-Sendrab), is an NK3 receptor antagonist that was initially developed for the treatment of schizophrenia and other central nervous system (CNS) disorders. In August 2005, during a review of its portfolio of research and development, the company announced it would discontinue further development of oxanetainetan. This followed the company's decision to discontinue development of eplerenserine for the treatment of schizophrenia. Oxanetainetan is a highly bioavailable, oral, blood-brain barrier-crossing, non-peptide neurokinin/tachykinin 3 receptor (NK1 receptor; NK3R; NK-3R) antagonist, potentially used to treat vasomotor symptoms (VMS) in menopausal women and men undergoing androgen deprivation therapy (ADT), and to inhibit the production of certain hormones. After oral administration, oxanelenthal targets and competitively binds to NK3R in the central nervous system (CNS), thereby blocking its activity and inhibiting NK3R-mediated signal transduction, potentially preventing certain menopausal symptoms, such as hot flashes and vasomotor symptoms (VMS) caused by androgen deficiency in men. Neurokinin-mediated signal transduction may be enhanced during hormone deficiency and may lead to hot flashes. Furthermore, oxanelenthal may inhibit the secretion of multiple hormones, such as testosterone, luteinizing hormone (LH), and follicle-stimulating hormone (FSH), by inhibiting NK3R. By inhibiting testosterone production, oxanelenthal may inhibit the proliferation of hormone-sensitive prostate cancer. Drug Indications It may be used to treat schizophrenia, depression, and visceral pain. Mechanism of Action The mechanism of action of oxanelenthal is currently unclear. Multiple preclinical data suggest that activation of the NK3 receptor can enhance the release of biogenic amines, including dopamine and serotonin. NK3 receptor antagonists block the activation of these systems mediated by NK3 receptors.

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Pharmacodynamics
Oxanetainment is a neurokinin-3 (NK3) receptor antagonist. Preliminary clinical trials have shown that oxanetainment is superior to placebo in overall efficacy assessments and positive symptom indicators for schizophrenia.

C35H41CL2N3O2

606.63

605.258

160492-56-8

(S)-Osanetant;182621-58-5

219077

White to off-white solid powder

1.25g/cm3

727.9ºC at 760mmHg

394ºC

4.79E-21mmHg at 25°C

1.633

7.293

0

3

8

42

897

1

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

DZOJBGLFWINFBF-UMSFTDKQSA-N

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

N-[1-[3-[(3R)-1-benzoyl-3-(3,4-dichlorophenyl)piperidin-3-yl]propyl]-4-phenylpiperidin-4-yl]-N-methylacetamide

SR 142801; SR142801; SR-142801

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ~66.67 mg/mL (~109.90 mM)

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.

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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.

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 (Please use freshly prepared in vivo formulations for optimal results.)