Tachykinnin - Receptor Antagonists

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A5330 N-Acetyl-L-tryptophan 3,5-bis(trifluoromethyl)benzyl ester ≥99% (TLC), powder Competitive substance P receptor antagonist. It is approximately 1000-fold more potent at cloned human NK-1 receptors than at cloned human NK-2 and NK-3 receptors; and approximately 200-fold more potent at human NK-1 receptors than at rat NK-1 receptors. The IC50 for the human NK-1 receptor expressed in CHO cells is approximately 2 nM.
human ... TACR1(6869)
PZ0136 CP-100263 dihydrochloride hydrate ≥97% (HPLC) CP-100263 is an NK-1 neurokinin receptor antagonist.
 
C9373 CP-96345 ≥98% (HPLC) CP-96345 is a selective NK1 antagonist. CP96345 inhibits substance P-induced salivation in the rat by classical in vivo bioassay, but did not inhibit NK2, NK3, or numerous other receptors.
 
F1183 FK888 hydrate Selective, high affinity tachykinin NK1 receptor antagonist.
 
L119 L-703,606 oxalate salt hydrate solid Potent and selective non-peptide NK-1 tachykinin receptor antagonist.
human ... TACR1(6869)
L138 L-733,061 hydrochloride solid Weak NK-1 tachykinin receptor antagonist; less active enantiomer of L-733,060 hydrochloride.
 
S5192 SB 222200 ≥98% (HPLC), solid Non-peptide NK3 tachykinin receptor antagonist.
SB 222200 is a 2-phenyl-4-quinolinecarboxamides and a selective, reversible and competitive antagonist of human NK-3 receptor that effectively crosses the blood-brain barrier. It inhibits the NK-3 receptor-induced miosis or pupil constriction in conscious rabbits.1,2
human ... TACR2(6865), TACR3(6870)
W103 WIN 51708 hydrate solid WIN 51708 hydrate is a non-peptide NK1 tachykinin receptor antagonist.
rat ... Tacr1(24807)
W104 WIN 62,577 solid Non-peptide NK1 tachykinin receptor antagonist.
human ... TACR1(6869)
rat ... Tacr1(24807)