antiobesity

Mifobate (SR-202) 是一种有效且特异性的 PPARγ拮抗剂，可选择性抑制噻唑烷二酮 (TZD) 诱导的 PPARγ 转录活性，IC50为140 μM，具有抗肥胖和抗糖尿病作用。

CB1 antagonist 4 是外周选择性大麻素受体1型受体拮抗剂。它减少精神病副作用的倾向。它对大脑的渗透率有限，以降低或防止 CNS 不良反应，并保留潜在的抗肥胖作用。

Orlistat (Tetrahydrolipstatin) 是一种脂肪酶 (lipase) 抑制剂，也是一种脂肪酸合成酶 (FASN) 抑制剂。Orlistat 具有促减肥的作用。

Cetilistat (ATL-962) 是胰腺脂肪酶 (pancreatic lipase) 抑制剂，能够抑制大鼠脂肪酶(IC50:54.8 nM)和人胰脂肪酶(IC50:5.95 nM)的活性，可用作有效的抗肥胖药。

1-Deoxynojirimycin (Moranoline) 是一种口服具有活性的 α-葡萄糖苷酶抑制剂。它具有降血糖、减肥和抗病毒的活性。它抑制餐后血糖，预防糖尿病。

KY-226 是选择性的，口服活性的和变构蛋白酪氨酸磷酸酶 1B 抑制剂，IC50=0.25 μM，且不激活 PPARγ 。它可以保护神经元免受脑缺血损伤。它通过增强胰岛素和瘦素信号传导发挥抗糖尿病和抗肥胖作用。

TGR5 Receptor Agonist 是一种TGR5(GPCR19)激动剂。

1-Deoxynojirimycin hydrochloride (Moranoline) 是一种口服有效的 α-葡萄糖苷酶抑制剂，具有降血糖、减肥和抗病毒的作用，可抑制餐后血糖，预防糖尿病。

Nomilin 是一种柠檬苦素类化合物，从柑桔类提取物中获得，是抗肥胖症和降糖药。

Tigogenin 是甾体皂甙元，普遍用于甾体类药物的合成。它能够阻碍小鼠骨髓基质细胞脂肪细胞分化，促使成骨细胞的分化。

5,7-Dimethoxyflavone 是一种 Kaempferia parviflora 的主要成分，具有抗肿瘤、抗肥胖及抗炎活性。它对细胞色素 P450 (CYP) 3As 具有抑制作用，也是抗乳腺癌蛋白 (BCRP) 抑制剂。

Anti-obesity agent 1 (compound 4) 显示出脂肪分解能力增强，因此展现出抗肥胖特性。

N-Aminopiperidine hydrochloride (Piperidin-1-amine hydrochloride) 是大麻素受体 1 拮抗剂 Rimonabant（一种抗肥胖剂）的代谢物(M1)。

Phloracetophenone (1-(2,4,6-Trihydroxyphenyl)ethanone) 是多叶姜黄中苯乙酮糖苷的糖苷配基部分，具有抗肥胖，降血脂和降低胆固醇作用，能够增强胆固醇 7α-羟化酶的活性。

(±)-Evodiamine是一种发现于Evodiae fructus的生物碱和topoisomerase I抑制剂，还能抑制脂肪细胞分化和糖尿病，可以下调IGF-1/HIF-1α和IL-6/STAT。(±)-Evodiamine是NF-kB激活的抑制剂，能抑制侵袭和促进凋亡，还能抑制TNF诱导的Akt活化。

LY-79771, a phenethanolamine antiobesity agent, can be effective in preventing fat regain following energy deprivation.

Ro 22-0654, a novel lipid synthesis inhibitor, has antiobesity effects.

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)

GLS1 Inhibitor-7 (compound 4d) 作为一种GLS1 抑制剂，表现出抑制浓度50%所需浓度（IC50）为46.7 μM，潜在用途涉及抗癌、抗衰老和抗肥胖。

Epitheaflagallin 3-O-gallate is a promising functional food material with potential antiobesity and antiperiodontal disease activities, suppressing tumor growth through [the] suppression of angiogenesis.

Erycibelline has antiobesity activity, it may be a useful therapeutic agent for body weight control by downregulating adipogenesis and lipogenesis.

Tachioside has antiobesity, antioxidant and α-glucosidase inhibitory activities, it decreases lipid content in 3T3-L1 adipocytes by inhibiting lipogenesis, shows antiobesity activities. Tachioside can inhibit nitric oxide production in lipopolysaccharides-stimulated RAW 264.7 cells with IC50 value of 12.14 μM.