Bombesin Receptors

Bombesin is a neuropeptide with many biological effects including hormone release, stimulation of pancreatic enzyme secretion, inhibition of gastric emptying and modulation of gastric acid secretion.

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.

ML-18 is a non-peptide bombesin receptor subtype-3 (BRS-3) antagonist with an IC50 of 4.8 μM.

MK-5046 is a novel BRS-3 agonist, binds to BRS-3 with high affinity (mouse Ki = 1.6 nM, human Ki = 25 nM).

Kuwanon G is a flavonoid compound that acts as an antagonist of the bombesin receptor. It demonstrates significant biological activities, including bactericidal, anti-tumor, anti-inflammatory, antioxidant, anti-atherosclerotic, and neuroprotective effects. Kuwanon G exhibits potent antibacterial activity against oral pathogens, particularly cariogenic and periodontal bacteria. Additionally, it induces apoptosis while inhibiting the proliferation, migration, and invasion of tumor cells, making it valuable for research in gastric cancer and atherosclerosis.

Bombesin receptor antagonist-1 functions as a selective antagonist for the bombesin receptors, exhibiting Ki values of 0.17 nM for the neurotide B (NMB) receptor and 20 nM for the gastrin-releasing peptide (GRP) receptor. This compound is instrumental in the investigation of various pathophysiological conditions, including cancer, depression, and eating disorders. Its precise modulation of bombesin receptors provides valuable insights into receptor signaling pathways and potential therapeutic targets in related diseases.

Kuwanon H is a flavonoid isolated from Morus alba that functions as a potent non-peptide antagonist of bombesin receptors. It selectively inhibits the binding of gastrin-releasing peptide to GRP-preferring receptors, exhibiting a Ki value of 290 nM in cellular assays. This compound is valuable for research applications involving cancer biology and neurobiology, particularly in studies focusing on receptor signaling pathways and their role in tumor growth and metastasis.

BIM-26226 is a selective antagonist of the gastrin-releasing peptide receptor (GRPR) and bombesin (BN) receptor, exhibiting an IC50 of 6 nM. This compound effectively inhibits BN- or GRP-stimulated amylase release with IC50 values of 0.3 nM and 0.2 nM, respectively. BIM-26226 shows high specificity for the GRP-preferring BN receptor subtype and does not interfere with the GRP receptor system. Additionally, it can induce the synthesis of somatostatin receptors while demonstrating no significant effect on tumor growth, making it valuable for research into neuropeptide signaling and related biological pathways.

ICI 216140 is a potent GRP/bombesin receptor 2 antagonist with an IC50 value of 2 nM. This compound effectively inhibits Bombesin-stimulated pancreatic amylase secretion and mitigates Bombesin-induced increases in blood pressure. ICI 216140 is valuable for research into the physiological roles of bombesin receptors and their implications in various pathophysiological conditions.

Ranatensin is an undecapeptide that acts as an agonist of the bombesin receptor. Isolated from amphibian skin, particularly from the frog Rana pipiens, ranatensin plays a crucial role in regulating blood pressure dynamics. It exhibits distinct biological activity without cross-tachyphylaxis with other peptides such as angiotensin amide, bradykinin, or norepinephrine, making it a valuable tool for cardiovascular research applications.

[D-Phe12,Leu14]-Bombesin is a potent antagonist of the Bombesin receptor. This compound exhibits key biological activity in blocking Bombesin-mediated signaling pathways, making it valuable for cancer research. It is utilized in studies focused on tumor growth and proliferation, particularly in neuroendocrine tumors and related conditions.

[D-Phe12]-Bombesin is a bombesin receptor antagonist with a Ki value of 4.7 μM. This compound effectively inhibits bombesin-induced amylase release, exhibiting an IC50 of 4 μM. It is valuable for research applications exploring the role of bombesin receptors in physiological and pathological processes, particularly in studies related to neuroendocrine signaling and cancer biology.

GRP (14-27) is a bombesin receptor ligand derived from human, porcine, and canine sources. This peptide displays specific binding properties to bombesin receptors, which is inhibited by guanosine triphosphate (GTP) and guanosine diphosphate (GDP), indicating a competitive mechanism of action. GRP (14-27) is useful in research applications focused on neuropeptide signaling and receptor interactions.

[D-Cys6,Asn7,D-Ala11,Cys14]-Bombesin (6-14) is a synthetic peptide that acts as a non-selective agonist for bombesin receptors. It exhibits favorable pEC50 values of 8.06 for the BB1 receptor, 8.69 for BB2, and 6.71 for BB3. This compound is valuable for research into various pathologies associated with bombesin receptors, including cancer and neurological disorders.