Current bombesin receptor nomenclature and general characteristics See text for references.

Receptor Code Mammalian Bombesin Receptor
Previous names NMB-R, NMB-preferring receptor GRP-R, GRP-preferring receptor BRS-3, bombesin receptor subtype 3
Cloned from mammals Human, rat, mouse, monkey Human, rat, mouse, monkey, chimpanzee, dog, sheep Human, rat, mouse, monkey, sheep
Gene location Chr 6p21 (human) Chr Xp22 (human) Chr Xq25 (human)
Structural information 390 aa (human) 384 aa (human) 399 aa (human)
Natural ligands NMB > GRP GRP > NMB Unknown (low-affinity NMB, GRP, all Bn natural related peptides)
Selective agonist NMB, NMB30 GRP [d-Tyr6,Apa-4Cl11,Phe13,Nle14]bombesin 6–14, Ac-Phe,Trp,Ala,His(tBzl),Nip,Gly,Arg-NH2
Selective antagonists PD 168368 [d-Phe6,Cpa14,ψ13–14]Bn6–14, JMV641, JMV594, BW2258U89, Ac-GRP20–26 methyl ester None
Principal transduction Gq/11 Gq/11 Gq/11
Preferred radioligand 125I-BH-[d-Tyr0]-NMB, 125I-[Tyr4]-Bn 125I-[GRP], 125I-[Tyr4]-Bn, 125I-[d-Tyr6]-Bn6–13 methyl ester 125I- [d-Phe6,β-Ala11,Phe13,Nle14]Bn6–14
Tissue functions CNS (regulate TSH release, satiety), GI tract (motility); regulate stress responses CNS (thermoregulation, regulate circadian rhythm, satiety); GI tract [hormone release, motility, regulate secretions (pancreas, gastric acid, islets)]; immunologic (chemoattractant, lymphocyte function); fetal development (lung) Regulate energy homeostasis, glucose/insulin regulation; satiety; lung development and response to injury: present myenteric/submucosa ganglia, cells of Cajal proposed to be involved in GI motility
Diseases Altered hypo-, hyperthyroidism; autocrine tumor growth factor (lung/colon tumors, carcinoids, others) Tumor growth effects–morphogen, autocrine growth factor (lung, colon, prostate, breast, head-neck tumors, others); lung diseases (bronchopulmonary dysplasia, tobacco injury) Tumor growth factor (lung, others)
Phenotype of knockout Reduced hypothermic effect to NMB; abnormal behaviors, dysregulation of thyroid-pituitary axis, altered CNS 5-HT system with stress Altered satiety, thermoregulation, abnormal behaviors, altered insulin release Mild obesity, hypertension, impaired glucose metabolism reduced metabolic rate, increased feeding behavior, altered lung response to injury
  • aa, amino acids