SDZ NKT 343 

SDZ NKT 343 is a selective, orally active NK₁ receptor antagonist with an IC₅₀ of 0.62 nM against human NK₁ receptor. SDZ NKT 343 has good analgesic activity^[1][2].

SDZ NKT 343 shows a markedly lower affinity at rat NK₁ receptors in whole forebrain membranes (IC₅₀=451+139 nM)^[1].
SDZ NKT 343 shows weak affinity to human NK₂ and NK₃ receptors in transfected Cos-7 cells (K_i of 0.52+0.04 μM and 3.4+1.2 μM respectively)^[1].

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

SDZ NKT 343 antagonized [Sar⁹]SP sulphone-evoked bronchoconstriction (70% reduction at 0.4 mg/kg, i.v.) in anaesthetized guinea-pigs^[1].

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

579.65

C₃₃H₃₃N₅O₅

180046-99-5

Room temperature in continental US; may vary elsewhere.

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

• [1]. Walpole CS, et al. Comparative, general pharmacology of SDZ NKT 343, a novel, selective NK1 receptor antagonist. Br J Pharmacol. 1998 May;124(1):83-92.  [Content Brief]

  [2]. Walpole C, et al. 2-Nitrophenylcarbamoyl-(S)-prolyl-(S)-3-(2-naphthyl)alanyl-N-benzyl-N - methylamide (SDZ NKT 343), a potent human NK1 tachykinin receptor antagonist with good oral analgesic activity in chronic pain models. J Med Chem. 1998 Aug 13;41(17)  [Content Brief]