neuromedin u

Neuromedin U,a 23-amino acid brain-gut peptide, regulates several important physiological functions through its cognate receptor NMUR2 in the central nervous system, including energy balance, stress response, and nociception.

Neuromedin U (rat) acetate 是一种 23 个氨基酸的脑肠肽。 Neuromedin U (NMU) 通过其在中枢神经系统中的同源受体 NMUR2 调节几种重要的生理功能，包括能量平衡、压力反应和伤害感受。

Neuromedin U-23 (NMU-23) is a neuropeptide involved in diverse biological processes, including smooth muscle contraction, energy homeostasis, and nociception.1It is an agonist of neuromedin-U receptor 1 (NMUR1; EC50= 0.17 nM for the human receptor in a calcium mobilization assay using HEK293 cells) and NMUR2 (EC50= ~1.4-2 nM for arachidonic acid release in CHO cells expressing the human receptor).2,3NMU-23 (1 μM) induces contractions in isolated rat colon smooth muscle strips.4It decreases body weight and food intake and increases core body temperature in mice when administered at a dose of 36 μg/animal.5Intrathecal administration of NMU-23 decreases the mechanical pain threshold in the von Frey test in rats.6 1.Mitchell, J.D., Maguire, J.J., and Davenport, A.P.Emerging pharmacology and physiology of neuromedin U and the structurally related peptide neuromedin SBr. J. Pharmacol.158(1)87-103(2009) 2.Szekeres, P.G., Muir, A.I., Spinage, L.D., et al.Neuromedin U is a potent agonist at the orphan G protein-coupled receptor FM3J. Biol. Chem.275(27)20247-20250(2000) 3.Hosoya, M., Moriya, T., Kawamata, Y., et al.Identification and functional characterization of a novel subtype of neuromedin U receptorJ. Biol. Chem.275(38)29528-29532(2000) 4.Brighton, P.J., Wise, A., Dass, N.B., et al.Paradoxical behavior of neuromedin U in isolated smooth muscle cells and intact tissueJ. Pharmacol. Exp. Ther.325(1)154-164(2008) 5.Peier, A., Kosinski, J., Cox-York, K., et al.The antiobesity effects of centrally administered neuromedin U and neuromedin S are mediated predominantly by the neuromedin U receptor 2 (NMUR2)Endocrinology150(7)3101-3109(2009) 6.Yu, X.H., Cao, C.Q., Mennicken, F., et al.Pro-nociceptive effects of neuromedin U in ratNeuroscience120(2)467-474(2003)

Neuromedin U (NMU) is a neuropeptide first demonstrated to drive smooth muscle contraction.1Translated as a 174 amino acid propeptide, NMU is cleaved to different lengths in different animals. It has diverse receptor-mediated rolesin vivo, as it regulates feeding, vasoconstriction, nociception, and bone remodeling and contributes to obesity, cancer and septic shock.2,2NMU-25 is the active form of NMU in humans. It binds with high affinity to receptors on human left ventricle and coronary artery (KDs = 0.26 and 0.11 nM, respectively), eliciting endothelium-independent vasoconstriction.3NMU-25 also suppresses glucose-stimulated insulin secretion in human islets, and this effect is lost in NMU R165W mutants, resulting in early-onset obesity.4 1.Mitchell, J.D., Maguire, J.J., and Davenport, A.P.Emerging pharmacology and physiology of neuromedin U and the structurally related peptide neuromedin SBritish Journal of Pharmacology15887-103(2009) 2.Greenwood, H.C., Bloom, S.R., and Murphy, K.G.Peptides and their potential role in the treatment of diabetes and obesityRev.Diabet.Stud.8(3)355-368(2011) 3.Mitchell, J.D., Maguire, J.J., Kuc, R.E., et al.Expression and vasoconstrictor function of anorexigenic peptides neuromedin U-25 and S in the human cardiovascular systemCardiovascular Research81353-361(2009) 4.Alfa, R.W., Park, S., Skelly, K.R., et al.Suppression of insulin production and secretion by a decretin hormoneCell Metabolism21(2)323-333(2015)

Neuromedin U-25 (porcine) 是一类具有子宫刺激和升高血压作用的肽。

Neuromedin U, rat TFA is a 23-amino acid brain-gut peptide.

Neuromedin U-25 human是Neuromedin U在人体内的活性形式。Neuromedin U-25 human抑制葡萄糖刺激的胰岛素分泌，导致早发性肥胖。同时，Neuromedin U-25在人血管床中充当血管收缩剂。

3'-Methoxyflavonol 是一种神经介肽 U 2 受体的选择性激动剂。

Neuromedin S (human) 是包含33个氨基酸的神经肽，作为G 蛋白偶联受体 (GPCR) FM-4 TGR-1的内源性配体，在大脑中被鉴定，并对神经调节素 U (NMU) 受体 2 (NMUR2)调节体重稳态具有调控作用。

NY0116是一种神经调节肽U受体2 (NMUR2) 激动剂，hNMUR1的EC50值为27.76 μM，hNMUR2的EC50值为13.61 μM。NY0116降低cAMP，同时在稳定表达NMUR2的HEK293细胞中刺激钙信号传导。

Potent, endogenous neuromedin U receptor agonist (EC50 values are 65 and 91 pM at NMU1 and NMU2 respectively). Induces phase shifts in the circadian rhythm of locomotor activity following i.c.v. administration. Potent endogenous anorexigenic peptide.

CPN-267 (compound 7b) TFA 是一种选择性刺激神经介质 U 受体 1 (NMUR1) 的激动剂，EC50为0.25 nM。CPN-267 TFA 能抑制小鼠体重增加，适用于肥胖研究。