Biological Activity
ki: 49 ±14 nm for neuromedin b-induced endpoint in hunmbr cellsneuromedin b, a mammalian peptide of the bombesinlike peptide family sharing amino acid homology with its amphibian counterpart ranatensin, elicits a diverse array of biological responses in central and peripheral tissues. bim 23042 [d-nal-cys-tyr- d-trp-lys-val-cys-nal-nh2] is a selective neuromedin b antagonist.
in vitro
bim 23042 has a l00-fold greater affinity for bb1 receptors than bb2 receptors. the submaximal mobilisation observed with neuromedin b (1 nm) was abolished by bim 23042 but restored with a subsequently higher concentration of neuromedin b (1 μm). bim 23042 competitively inhibited neuromedin b-induced endpoint in hunmbr cells with a ki of 49 ±14 nm [1].
References
[1] ryan rr, taylor je, daniel jl, cowan a. pharmacological profiles of two bombesin analogues in cells transfected with human neuromedin b receptors. eur j pharmacol. 1996 jun 13;306(1-3):307-14.
