204067-01-6

PD176252 is a potent antagonist of neuromedin-B preferring (BB1) and gastrin-releasing peptide-preferring (BB2) receptor with Kis of 0.17 nM and 1 nM for human BB1 and BB2 receptors, and 0.66 nM, 16 nM for Rat BB1 and BB2 receptors, respectively; PD176252 is also an agonist of N-Formyl peptide receptor1/2 (FPR1/FPR2), with EC50s of 0.31 and 0.66 μM in HL-60 cells.

Non-peptide gastrin-releasing peptide receptor (GRP-R, BB 2 ) and neuromedin B receptor (NMB-R, BB 1 ) antagonist (K i values are 0.17 and 1.0 nM for BB 1 and BB 2 respectively). Inhibits proliferation of rat C6 glioma cells (IC 50 = 2 μ M) and inhibits NCI-H1299 xenograft proliferation in nude mice (IC 50 = 5 μ M).

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[1] Ashwood V, et al. PD 176252--the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist. Bioorg Med Chem Lett. 1998 Sep 22;8(18):2589-94. DOI:10.1016/s0960-894x(98)00462-4
[2] Schepetkin IA, et al. Gastrin-releasing peptide/neuromedin B receptor antagonists PD176252, PD168368, and related analogs are potent agonists of human formyl-peptide receptors. Mol Pharmacol. 2011 Jan;79(1):77-90. DOI:10.1124/mol.110.068288
[3] Moody TW, et al. Nonpeptide gastrin releasing peptide receptor antagonists inhibit the proliferation of lung cancer cells. Eur J Pharmacol. 2003 Aug 1;474(1):21-9. DOI:10.1016/s0014-2999(03)01996-4