SDZ NKT 343_product_DataBase

Bioactivity	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].
Invitro	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 (Ki of 0.52+0.04 μM and 3.4+1.2 μM respectively)[1].
In Vivo	SDZ NKT 343 antagonized [Sar9]SP sulphone-evoked bronchoconstriction (70% reduction at 0.4 mg/kg, i.v.) in anaesthetized guinea-pigs[1].
Name	SDZ NKT 343
CAS	180046-99-5
Formula	C33H33N5O5
Molar Mass	579.65
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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. [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)

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