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Bombesin Receptors(铃蟾肽受体)

Bombesin, a peptide of 14 amino acids, is an amphibian homolog to the mammalian gastrin-releasing peptide (GRP), that has been extensively studied as a targeting ligand for diagnosis and therapy of GRP positive tumors, such as breast, pancreas, lungs and prostate cancers. Bombesin binds to and activates G-protein coupled receptors, known as gastrin releasing peptide receptor (GRPR).

Bombesin, a tetradecapeptide isolated from the skin of the frog Bombina bombina, have shown broad spectrum of biological activities. The BBS activates three G protein-coupled receptors: bombesin receptor 1 (BB1), bombesin receptor 2 (BB2), and bombesin receptor 3 (BB3). BBS-like peptides-Neuromedin B (NB) and gastrin releasing peptide (GRP) are natural ligand of the BB1 and BB2 receptors, respectively.

In mammals, BBS receptors and BBS-like peptides are distributed in the Central Nervous System (CNS) including regions involved in the cardiorespiratory control.

The mammalian bombesin G-protein-coupled receptor subfamily comprises three structurally related members, the receptors for neuromedin B (NMBR or BB1), gastrin-releasing peptide (GRPR or BB2), and bombesin receptor subtype-3 (BRS-3 or BB3).

Bombesin receptor subtype-3 (BRS-3) is an orphan G protein-coupled receptor implicated in the regulation of energy homeostasis.

  1. Cat.No. 产品名称 Information
  2. GC64112 RC-3095 TFA RC-3095 TFA 是一种选择性蛙皮素 (bombesin)/胃泌素 (gastrin) 释放肽受体拮抗剂。RC-3095 TFA 作用于关节炎小鼠,通过减少胃氧化损伤来发挥保护作用。
  3. GC60619 BA 1 TFA BA 1 TFA 是铃蟾肽 (BB) 受体家族的有效激动剂。
  4. GC50215 BA 1 BA 1 是铃蟾肽 (BB) 受体家族的有效激动剂。
  5. GC38510 Kuwanon H Kuwanon H 是桑白皮中的黄酮类化合物,为非肽类蛙皮素受体 (bombesin receptor) 拮抗剂。Kuwanon H 可特异性抑制细胞内胃泌激素释放肽 CRP 与(GRP-preferring recepotr) 受体的结合,Ki 值为 290 nM。
  6. GC37072 RC-3095 RC-3095 是一种蛙皮素 (bombesin)/胃泌素 (gastrin) 释放肽受体拮抗剂。
  7. GC36404 Kuwanon G Kuwanon G 是从桑树中得到的黄酮类化合物,为蛙皮素受体 (bombesin receptor) 拮抗剂,具有杀菌作用。
  8. GC33152 ML-18 ML-18是一种抑制肺癌生长的非肽铃蟾肽受体亚型-3(BRS-3)拮抗剂。
  9. GC19413 MK-5046 MK-5046 是一种新型 BRS-3 激动剂,以高亲和力与 BRS-3 结合(小鼠 Ki = 1.6 nM,人 Ki = 25 nM)。
  10. GC17156 [D-Phe12,Leu14]-Bombesin Bombesin receptor antagonist
  11. GC17080 BIM 23042 Antagonist of neuromedin B receptor,selective
  12. GC14279 BIM 189 Bombesin antagonist
  13. GC15165 BIM 187 Bombesin/GRP receptor agonist
  14. GC14662 Litorin Litorin 是一种两栖类铃蟾肽衍生物,是铃蟾肽受体激动剂。
  15. GC15163 [D-Phe12]-Bombesin Bombesin receptor antagonist
  16. GC12707 Neuromedin B (porcine) Neuromedin B (porcine) (NMB) 是哺乳动物中铃蟾肽 (BN) 样肽家族的成员。
  17. GC16376 Neuromedin C (porcine) Mammalian bombesin-like neuropeptide
  18. GC11620 BIM 23127 Antagonist of neuromedin B receptor
  19. GC16415 GRP (human) GRP(人)(GRP)属于铃蟾肽样肽家族,不是经典的下丘脑-垂体调节激素,因为它在介导垂体激素释放中仅起到敷衍作用。
  20. GC16854 GRP (porcine) agonist for the gastrin-releasing peptide receptor (GRPR)
  21. GC14014 Bombesin Bombesin是一种十四肽,在胃泌素的释放和G蛋白受体的激活中起重要作用。
  22. GC13768 PD 176252 PD 176252 是一种有效的神经调节素-B 优先 (BB1) 和胃泌素释放肽优先 (BB2) 受体拮抗剂,对人 BB1 和 BB2 受体的 Kis 分别为 0.17 nM 和 1 nM,对大鼠 BB1 和 BB2 受体的 Kis 分别为 0.66 nM 和 16 nM BB2 受体,分别; PD 176252 也是 N-Formyl peptide receptor1/2 (FPR1/FPR2) 的激动剂,在 HL-60 细胞中的 EC50 为 0.31 和 0.66 μM。
  23. GC14908 Alytesin Amphibian bombesin-like peptide

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