Bombesin Receptor

PD 168368 is a novel, potent, competitive and selective nonpeptide neuromodulin B receptor (NMB-R) antagonist with inhibitory effects on the gastrin-releasing peptide receptor (GRPR).PD 168368 is a potent mixed agonist of FPR1 FPR2 FPR3.

Litorin acetate, an amphibian bombesin peptide derivative, is an bombesin receptor agonist. It stimulates the contraction of smooth muscle, stimulates gastrin, gastric acid, and pancreatic secretion, and suppresses the nutriment in vivo.

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

CD80-IN-3 is a potent CD80 inhibitor and inhibits CD80/CD28 interaction (Kd: 125 nM; EC50: 630 nM).

PD176252 is a potent BB1 and BB2 antagonist with inhibitory effects on BB1 and BB2 receptors.PD176252 acts as a small molecule GRPR inhibitor and FPR1 FPR2 agonist to inhibit the growth and proliferation of a variety of cancer cells.

1. Kuwanon G (Moracenin B) as dual inhibitors of PTP1B and α-glucosidase enzymes, as well as insulin sensitizers, it may potentially be utilized as an effective treatment for Type II diabetes mellitus. 2. Kuwanon G has anti-inflammatory activity, it can attenuate atherosclerosis through inhibiting foam cell formation and inflammatory response. 3. Kuwanon G is a potent inhibitor of Mycobacterium tuberculosis protein tyrosine phosphatase B. 4. Kuwanon G shows acetylcholinesterase (AChE) and butyrylcholinesterase(BChE) inhibitory activities, it may be a promising candidate for preventive and therapeutic agents for Alzheimer's disease. 5. Kuwanon G prevents the pathological progression of allergic asthma through the inhibition of lung destruction by inflammation and immune stimulation. 6. Kuwanon G has antibacterial activity against oral pathogens. 7. Kuwanon G is a specific antagonist for the GRP-preferring receptor and can be useful for studying the physiological and pathological role of GRP.

Bombesin acetate is a 14-amino acid peptide originally isolated from the skin of the European fire-bellied toad (Bombina bombina). It has two known homologs in mammals called neuromedin B and gastrin-releasing peptide.

BA 1 acetate is a potent bombesin receptor agonist (IC50 values are 0.26, 1.55 and 2.52 nM for BB1, BB2 and BB3 respectively). Enhances glucose transport in obese and diabetic primary myocytes. Also stimulates NCI-H1299 lung cancer cell proliferation in v

Kuwanon H, and possibly kuwanon G also, are specific antagonists for the gastrin-releasing peptide (GRP) -preferring receptor and can be useful for studying the physiological and pathological role of GRP.

[D-Phe12]-Bombesin acetate inhibits bombesin-stimulated secretion.

[D-Phe12,Leu14]-Bombesin acetate inhibits bombesin-stimulated secretion.

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

GRP (14-27) (human, porcine, canine) serves as a ligand for bombesin receptors, with specific binding inhibited by GTP and GDP, but unaffected by GMP [1].

GB-6, a short linear peptide that selectively binds to the gastrin releasing peptide receptor (GRPR), shows potential as a high-contrast imaging probe due to its tumor selectivity and specific accumulation. Overexpression of GRPR in pancreatic cancer enables GB-6, when labeled with near-infrared (NIR) fluorescent dyes or the radionuclide technetium-99m (99mTc), to serve as an effective agent for tumor visualization. Demonstrating excellent in vivo stability, GB-6 yields tumor to pancreatic and intestinal fluorescence signal ratios of 5.2 and 6.3, respectively, in SW1990 subcutaneous xenograft models. Its rapid tumor targeting capability and precise tumor boundary delineation signify GB-6's extensive potential for clinical applications [1].

RC-3095 TFA (RC-3095 (TFA)) is a bombesin/gastrin-releasing peptide (BN/GRP) antagonist with potential anticancer activity.