GR 87389 

GR 87389 is a potent NK2 receptor antagonist. GR 87389 antagonized GA 64349-induced smooth muscle strips contractions in a competitive manner in the human detrusor, prostate and prostatic urethra^[1][2].

GR 87389 is a non-peptide and peptide tachykinin antagonist with K_i values of 4.0, 5.2, and 14 nM for hippocampus, urinary bladder and duodenum, respectively^[1].
GR 87389 (30-300 nM) antagonized GA 64349-induced smooth muscle strips contractions in human isolated detrusor, prostate and prostatic urethra^[2].

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

900.07

C₄₇H₆₅N₉O₉

141663-86-7

{Boc}-AA-{D-Trp}-F-{D-Pro}-P-{Nle}-NH2

O=C(N1[C@H](CCC1)C(N2[C@@H](CCC2)C(N[C@H](C(N)=O)CCCC)=O)=O)[C@H](CC3=CC=CC=C3)NC([C@H](NC([C@H](C)NC([C@H](C)NC(OC(C)(C)C)=O)=O)=O)CC4=CNC5=CC=CC=C45)=O

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• [1]. Saffroy M, et, al. Presence of NK2 binding sites in the rat brain. J Neurochem. 2001 Dec;79(5):985-96.  [Content Brief]

  [2]. Palea S, et, al. Pharmacological characterization of tachykinin NK2 receptors on isolated human urinary bladder, prostatic urethra and prostate. J Pharmacol Exp Ther. 1996 May;277(2):700-5.  [Content Brief]