Osanetant hydrate

Osanetant is a neurokinin-3 (NK3) receptor antagonist (Ki = 0.21 nM in CHO cells expressing the human receptor).1 It is selective for NK3 over NK1 and NK2 receptors (Kis = >100 and 0.02 µM, respectively).2 Osanetant inhibits contractions and acetylcholine release induced by neurokinin B (Item No. 24542) in isolated guinea pig ileal strips in a concentration-dependent manner.1 It inhibits ovalbumin-induced increases in bronchoalveolar lavage fluid (BALF) neutrophil, eosinophil, and lymphocyte infiltration in an ovalbumin-sensitized mouse model of allergic asthma.3 Osanetant (5 and 10 mg/kg) increases the duration of social interaction, as well as reduces immobility time in the tonic immobility test, indicating anxiolytic-like and antidepressant-like activities, respectively, in gerbils.4WARNING This product is not for human or veterinary use.

[1] X. EMONDS-ALT . SR 142801, The first potent non-peptide antagonist of the tachykinin NK3 receptor[J]. Life sciences, 1994, 56 1: Pages PL27-PL32. DOI: 10.1016/0024-3205(94)00413-m
[2] GUY GRIEBEL  Sandra B. Is there still a future for neurokinin 3 receptor antagonists as potential drugs for the treatment of psychiatric diseases[J]. Pharmacology & Therapeutics, 2012, 133 1: Pages 116-123. DOI: 10.1016/j.pharmthera.2011.09.007
[3] SOAZIG NÉNAN . Inhibition of inflammatory cell recruitment by the tachykinin NK3-receptor antagonist, SR 142801, in a murine model of asthma[J]. European journal of pharmacology, 2001, 421 3: Pages 201-205. DOI: 10.1016/s0014-2999(01)01036-6
[4] N. SALOMÉ. Selective blockade of NK2 or NK3 receptors produces anxiolytic- and antidepressant-like effects in gerbils[J]. Pharmacology Biochemistry and Behavior, 2006, 83 4: Pages 533-539. DOI: 10.1016/j.pbb.2006.03.013