muscle strips

CP-640186 是一种有效的乙酰辅酶 A 羧化酶 (ACC)抑制剂，抑制大鼠肝脏 ACC1 和大鼠骨骼肌 ACC2 的 IC50分别为 53 nM 和 61 nM。

CP-640186 hydrochloride (CP 640186 HCl) 是膜渗透性的乙酰辅酶A 羧化酶（ACC）抑制剂，抑制大鼠肝脏ACC1和大鼠骨骼肌ACC2的IC50为53 nM 和61 nM。

KT-362 fumarate 是一种新型化合物，可作为钙通道、钾通道和钠通道的拮抗剂.KT-362 fumarate 通过影响心房肌肉细胞内钙动员导致血管舒张。KT-362 fumarate 对兔子的股动脉和基底动脉条有放松作用。

BMS-195270 是一种具有组织特异性的大鼠膀胱肌张力和自发收缩抑制剂，能够在膀胱离体模型中抑制离体大鼠膀胱组织条的 Carbachol 引发的张力,抑制钙离子通量。

CHIR98014 is a reversible, cell-permeable inhibitor of GSK3α and GSK3β (IC50s: 0.65 and 0.58 nM). Through its effects on GSK3, CHIR98014 stimulates glycogen synthase in cells (EC50: 106 nM), potentiates insulin-dependent glucose transport in isolated musc

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)

Obestatin is a 23 amino acid peptide hormone with a conserved C-terminal glycine residue and amidation site that is formed by cleavage of the ghrelin and obestatin prepropeptide.1It binds to the orphan receptor GPR39 (Kd= 1 nM) and stimulates cAMP production in CHO and HEK293 cells overexpressing human GPR39. Obestatin inhibits contraction of isolated mouse jejunum muscle strips induced by ghrelin .In vivo, obestatin (12.5-1,000 nmol/kg) suppresses food intake in a time- and dose-dependent manner and reduces body weight gain and gastric emptying in mice. Obestatin (0.22 g per animal) also reduces food intake and glucose response without affecting plasma insulin responses in fasted high-fat diet fed mice.2 1.Zhang, J.V., Ren, P.C., Avsian-Kretchmer, O., et al.Obestatin, a peptide encoded by the ghrelin gene, opposes ghrelin's effects on food intakeScience310(5750)996-999(2005) 2.Subasinghage, A.P., Green, B.D., Flatt, P.R., et al.Metabolic and structural properties of human obestatin {1-23} and two fragment peptidesPeptides31(9)1697-1705(2010)

Lipoxin A5 (LXA5) is produced by enzymatic transformation of EPA by leukocytes. LXA5 slowly contracts pulmonary parenchymal strips from guinea pig with similar potency to that of LXA4 and LXB4. However, LXA5 does not exert the vasodilatory effects on aortic smooth muscle exhibited by LXA4 and LXB4.

Leukotriene C4 (LTC4) is the parent cysteinyl-leukotriene produced by the LTC4 synthase-catalyzed conjugation of glutathione to LTA4. LTC4 is produced by neutrophils, macrophages, and mast cells, and by transcellular metabolism in platelets. It is one of the constituents of slow-reacting substance of anaphylaxis (SRS-A) and exhibits potent smooth muscle contracting activity. LTC4-induced bronchoconstriction and enhanced vascular permeability contribute to the pathogenesis of asthma and acute allergic hypersensitivity. The concentration of LTC4 required to produce marked contractions of lung parenchymal strips and isolated tracheal rings is about 1 nM. LTC4 methyl ester is a more lipid soluble form of LTC4. The biological activity of LTC4 methyl ester has not been reported.

GR 87389 是一种有效的NK2受体拮抗剂。GR 87389 以竞争性方式拮抗 GA 64349 诱导的人类逼尿肌、前列腺和前列腺尿道平滑肌条收缩。

BNP-32（Brain natriuretic peptide-32）是心血管激素前体proBNP的肽段，能够结合大鼠血管平滑肌上的利钠肽受体（IC50 = 7.3 nM），并在同样的细胞中促进cGMP积累（EC50 = 170 nM）。BNP-32还能使经去甲肾上腺素预收缩的孤立大鼠主动脉条带松弛（EC50 = 6.7 nM），当以3 µg kg的剂量给药时，能增加大鼠的尿量和尿液电解质排泄，并诱导低血压。

2-Chloroadenosine 5-triphosphate (2-chloro ATP), an analog of ATP and adenine nucleotide, functions as an antagonist of the purinergic P2Y1 receptor, inhibiting ADP-induced intracellular calcium mobilization in Jurkat cells with a Ki value of 2.3 µM. Additionally, 2-chloro ATP acts as an agonist of purinergic P2X receptors, demonstrated by inducing inward currents in HEK293 cells expressing either human bladder smooth muscle or rat PC12 receptor forms, with EC50 values of 0.5 and 2.5 µM, respectively. It also triggers relaxation in precontracted isolated guinea pig taenia caeci strips in a concentration-dependent fashion. Furthermore, 2-chloro ATP has been employed in research to investigate the substrate specificity of cyclic nucleotide-dependent protein kinases, including protein kinase A (PKA) and PKG.

CL 316243 free acid 在大鼠心脏和比目鱼肌的IC 50 值分别为0.6 μM 和1 μM。此化合物还能抑制大鼠逼尿肌条的自发收缩，在浓度依赖性的条件下，其平均浓度在抑制最大反应50%时为2.65 nM。