Bioactivity | 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 Neuromedin B (HY-P0241), ICI 216140 and DPDM-bombesin ethylamide-induced Ca2+ release[1][2][3]. |
Invitro | BIM 23042 (5 μM) 在 huNMBR 细胞中竞争性抑制 Neuromedin B 诱导的 [3H] 花生四烯酸释放,Ki 为 49 nM[1]。 |
In Vivo | BIM 23042 (10μg; 静脉给药; 单次推注) 可减轻神经源性肿胀和热和机械致敏[2]。 Animal Model: |
Name | BIM 23042 |
CAS | 111857-96-6 |
Shortening | {DNal}-CY-{DTrp}-KVC-{Nal}-NH2 (Disulfide bridge:Cys2-Cys7) |
Formula | C63H73N11O9S2 |
Molar Mass | 1192.45 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. R R Ryan, et al. 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. [2]. Santosh K Mishra, et al. A nociceptive signaling role for neuromedin B. J Neurosci. 2012 Jun 20;32(25):8686-95. [3]. M Orbuch, et al. Discovery of a novel class of neuromedin B receptor antagonists, substituted somatostatin analogues. Mol Pharmacol. 1993 Oct;44(4):841-50. |