Talnetant hydrochloride  (Synonyms: SB 223412 hydrochloride; SB 223412-A)

Talnetant (SB 223412) hydrochloride is a selective, competitive, brain-permeable NK3 receptor antagonist with a K_i of 1.4 nM in hNK-3-CHO cells. Talnetant hydrochloride is 100-fold more selective for hNK-3 relative to the hNK-2 receptor and has no affinity for hNK-1. Talnetant hydrochloride can be used in schizophrenia-related studies^[1][2][3].

Talnetant (SB 223412) (0.1-1 μM) hydrochloride can reduce the accumulation of NKB-induced IP in U-2OS cells expressing the human NK3 receptor^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Talnetant (SB 223412) hydrochloride (0.5-2 mg/kg iv, 2min pretreatment) can inhibit the miosis induced by senktide (25µg, iv) in a dose-dependent manner with an ED₅₀ of 0.44mg/kg in conscious rabbits^[1].
Talnetant (SB 223412) hydrochloride (i.p., 1-100 mg/kg, 1 h) can significantly attenuate senktide-induced "wet dog wagging" behavior in a dose-dependent manner, significantly increase extracellular dopamine and norepinephrine in the medial prefrontal cortex and reduce haloperidol-induced increases in dopamine levels in the vomeronasal nucleus of freely moving guinea pigs^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

418.92

C₂₅H₂₃ClN₂O₂

204519-66-4

盐酸他奈坦

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Giardina GA, et al. Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 2. Identification of (S)-N-(1-phenylpropyl)-3-hydroxy-2-phenylquinoline-4-carboxamide (SB 223412). J Med Chem. 1999 Mar 25;42(6):1053-  [Content Brief]

  [2]. Houghton LA, et al. Effect of the NK(3) receptor antagonist, talnetant, on rectal sensory function and compliance in healthy humans. Neurogastroenterol Motil. 2007 Sep;19(9):732-43.  [Content Brief]

  [3]. Dawson LA, et al. In vitro and in vivo characterization of the non-peptide NK3 receptor antagonist SB-223412 (talnetant): potential therapeutic utility in the treatment of schizophrenia. Neuropsychopharmacology. 2008 Jun;33(7):1642-52.  [Content Brief]