Date published: 2026-5-19

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PD 176252 (CAS 204067-01-6)

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Alternate Names:
(S)-N-[[1-(5-Methoxy-2-pyridinyl)cyclohexyl]methyl]-α-methyl-α-[[[-(4-nitrophenyl)amino]carbonyl]amino-1H-indole-3-propanamide
Application:
PD 176252 is a GRPR and NMBR inhibitor
CAS Number:
204067-01-6
Purity:
≥98%
Molecular Weight:
584.67
Molecular Formula:
C32H36N6O5
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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PD 176252 is an organic compound known for its role as a potent and selective antagonist of the neurokinin-1 (NK1) and neurokinin-2 (NK2) receptors, which are part of the tachykinin receptor family implicated in numerous physiological processes. This chemical operates by inhibiting the binding of the natural ligands, substance P (for NK1) and neurokinin A (for NK2), to their respective receptors, thereby modulating the signaling pathways associated with these neurotransmitters. Due to its high specificity and efficacy in blocking NK1 and NK2 receptors, PD 176252 is extensively utilized in neurobiological research to dissect the complex roles of these receptors in pain transmission, neurogenic inflammation, and the modulation of mood and anxiety. By acting as a tool to inhibit NK1 and NK2 receptor activities, PD 176252 allows scientists to explore the fundamental mechanisms underlying the neurotransmission and physiological responses mediated by these tachykinins, contributing significantly to our understanding of their function in the nervous system.


PD 176252 (CAS 204067-01-6) References

  1. Role of bombesin-related peptides in the mediation or integration of the stress response.  |  Merali, Z., et al. 2002. Cell Mol Life Sci. 59: 272-87. PMID: 11915944
  2. Nonpeptide gastrin releasing peptide receptor antagonists inhibit the proliferation of lung cancer cells.  |  Moody, TW., et al. 2003. Eur J Pharmacol. 474: 21-9. PMID: 12909192
  3. Gastrin-releasing peptide receptor mediates activation of the epidermal growth factor receptor in lung cancer cells.  |  Thomas, SM., et al. 2005. Neoplasia. 7: 426-31. PMID: 15967120
  4. Bombesin receptors as a novel anti-anxiety therapeutic target: BB1 receptor actions on anxiety through alterations of serotonin activity.  |  Merali, Z., et al. 2006. J Neurosci. 26: 10387-96. PMID: 17035523
  5. Role of gastrin-releasing peptide and neuromedin B in anxiety and fear-related behavior.  |  Bédard, T., et al. 2007. Behav Brain Res. 179: 133-40. PMID: 17335915
  6. EGF receptor activation by GPCRs: an universal pathway reveals different versions.  |  Liebmann, C. 2011. Mol Cell Endocrinol. 331: 222-31. PMID: 20398727
  7. Gastrin-releasing peptide promotes the growth of HepG2 cells via EGFR-independent ERK1/2 activation.  |  Li, X., et al. 2010. Oncol Rep. 24: 441-8. PMID: 20596631
  8. Expression of gastrin-releasing peptide is increased by prolonged stretch of human myometrium, and antagonists of its receptor inhibit contractility.  |  Tattersall, M., et al. 2012. J Physiol. 590: 2081-93. PMID: 22411014
  9. Gastrin-releasing peptide acts via postsynaptic BB2 receptors to modulate inward rectifier K+ and TRPV1-like conductances in rat paraventricular thalamic neurons.  |  Hermes, ML., et al. 2013. J Physiol. 591: 1823-39. PMID: 23359674
  10. Gastrin-Releasing Peptide Receptor Targeting in Cancer Treatment: Emerging Signaling Networks and Therapeutic Applications.  |  Laukkanen, MO. and Castellone, MD. 2016. Curr Drug Targets. 17: 508-14. PMID: 26424393
  11. Structural Determinants in the Binding of BB2 Receptor Ligands: In Silico, X-Ray and NMR Studies in PD176252 Analogues.  |  Carrieri, A., et al. 2017. Curr Top Med Chem. 17: 1599-1610. PMID: 27823569
  12. Structure-activity relationship study towards non-peptidic positron emission tomography (PET) radiotracer for gastrin releasing peptide receptors: Development of [18F] (S)-3-(1H-indol-3-yl)-N-[1-[5-(2-fluoroethoxy)pyridin-2-yl]cyclohexylmethyl]-2-methyl-2-[3-(4-nitrophenyl)ureido]propionamide.  |  Lacivita, E., et al. 2017. Bioorg Med Chem. 25: 277-292. PMID: 27863916
  13. Preclinical Evaluation of NHS-Activated Gold Nanoparticles Functionalized with Bombesin or Neurotensin-Like Peptides for Targeting Colon and Prostate Tumours.  |  Chilug, LE., et al. 2020. Molecules. 25: PMID: 32722221
  14. PD 176252--the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist.  |  Ashwood, V., et al. 1998. Bioorg Med Chem Lett. 8: 2589-94. PMID: 9873586

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

PD 176252, 1 mg

sc-204171A
1 mg
$100.00

PD 176252, 5 mg

sc-204171
5 mg
$295.00