Abstract
We examined the effect of two des-Met-bombesin analogues, [(CH 3) 2CHCO-His-Trp-Ala-Val- d-Ala-His-Leu-NHCH 3] (ICI 216140) and [ d-Phe 6,des-Met 14]bombesin(6–14) ethylamide (DPDM-bombesin ethylamide), on neuromedin B-induced Ca 2+ and [ 3H]arachidonate release in BALB 3T3 cells transfected with human neuromedin B receptors. ICI 216140 and DPDM-bombesin ethylamide both stimulated Ca 2+ mobilisation in a concentration-dependent manner but were less potent and efficacious than neuromedin B. BIM 23042 [ d-Nal-Cys-Tyr- d-Trp-Lys-Val-Cys-Nal-NH 2], a selective neuromedin B antagonist and [ d-Arg 1, d-Phe 5, d-Trp 7.9,Leu 11]substance P, a broad-spectrum peptide receptor antagonist inhibited neuromedin B-, ICI 216140- and DPDM-bombesin ethylamide-induced Ca 2+ release. Pretreatment of cells with either des-Met-bombesin analogue attenuated neuromedin B-induced Ca 2+ elevations, suggesting similar agonist-sensitive Ca 2+ pools. The pharmacological profiles revealed from the [ 3H]arachidonate assay were similar, although ICI 216140 was less potent and efficacious than DPDM-bombesin ethylamide. The data suggest that ICI 216140 and DPDM-bombesin ethylamide behave as agonists at the neuromedin B receptor, perhaps as a consequence of neuromedin B receptor overexpression.
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