Uses
BIM 23042, a certain somatostatin (SS) octapeptide analogue, is a selective neuropeptide neuromedin B receptor (NMB-R, BB1) antagonist. BIM 23042 has 100-fold lower affinity for gastrin-releasing peptide (GRP) receptor (BB2). BIM 23042 inhibits NeuromedinB(HY-P0241), ICI 216140 and DPDM-bombesin ethylamide-induced Ca2+ release[1][2][3].
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].
in vivo
BIM 23042 (10 μg; IV; a single bolus) attenuates neurogenic swelling and thermal and mechanical sensitization[2].
| Animal Model: | Mice were 25-30 g male C57BL/6[2] |
| Dosage: | 10 μg |
| Administration: | IV; a single bolus |
| Result: | Attenuated neurogenic swelling and thermal and mechanical sensitization. |
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.
