intake

Nociceptin (1-13), amide 是一种 ORL1 (OP4) 受体激动剂，与大鼠前脑膜结合的 Ki 为 0.75 nM，对小鼠输精管的 pEC50 为 7.9。

HS024 是一种选择性的MC4受体拮抗剂，可增加食物摄入，对 MC4、MC5、MC3 和 MC1 的Ki 分别为 0.29、3.29、5.45 和 18.6 nM。

[D-Trp34]-Neuropeptide Y Acetate 是有效的、选择性的神经肽 Y (NPY) Y5 受体激动剂，在 NPY Y1，Y2，Y4 和 y6 受体上的效力较低。[D-Trp34]-Neuropeptide Y Acetate 可以显著增加大鼠的食物摄入量。

M40 acetate(143896-17-7 free base) 是一种有效的、非选择性的甘丙肽受体拮抗剂（GAL1 和 GAL2 的 Ki 值分别为 1.82 和 5.1 nM），在体外抑制大鼠脑中甘丙肽 (1-29) 的结合 (IC50 = 3 - 15 nM)。减弱氟西汀的抗抑郁作用并阻止甘丙肽诱导的体内食物摄入。在剂量 > 100 nM 时，对外周 GAL2 受体也表现出较弱的部分激动剂活性。

HS 014 acetate(207678-81-7 free base) 是一种有效的选择性黑皮质素 MC4 受体拮抗剂（克隆的人 MC4、MC1、MC3 和 MC5 受体的 Ki 值分别为 3.16、108、54.4 和 694 nM）。体内中枢给药后增加大鼠的食物摄入和小鼠的伤害感受。还抑制室旁下丘脑中 IL-1β 诱导的 Fos 表达。

Obestatin (rat) acetate 是 G 蛋白偶联受体 39 (GPR39) 的内源性配体。它具有抗炎、抗心肌梗塞和抗氧化特性。 它抑制食物摄入，抑制空肠收缩，并减少体重增加。

β-Endorphin (β-EP) is an endogenous opioid neuropeptide with diverse biological activities. It is produced via piomelanocortin cleavage in the pituitary gland, hypothalamus, and in lymphocytes, then migrates to its sites of action which include plasma, gut, skin, placenta, cerebrospinal fluid, and cardiac tissues. β-EP induces concentration-dependent decreases in electrically stimulated contraction of the mouse vas deferens that can be reversed by the μ-opioid antagonist CTP and δ-opioid antagonist ICI 174,864. In vivo, β-EP (5 μg, i.c.v.) slows gastrointestinal transit in mice. β-EP (0.5 or 5 μg, i.c.v.) stimulates food intake in rats for 4 to 6 hours, however, this effect is not prolonged with continuous infusion. It antagonizes the appetite-suppressive effects of α-melanocyte-stimulating hormone (α-MSH) for the first three days post administration. β-EP also reduces paralytic demyelination induced by the murine coronavirus MHV-JHM in immunocompetent, but not irradiated or immune-incompetent, mice and rats.

Peptide YY (PYY) is a 36-amino acid peptide and anorectic gut hormone agonist for the neuropeptide Y receptors Y1, Y2, Y5, and Y6 with EC50 values of 0.7, 0.58, 1, and 0.8 nM, respectively, for supression of forskolin-induced cAMP accumulation. PYY is cleaved in vivo to PYY (3-36) . Release of PYY occurs postprandially in proportion to calorie intake from intestinal enteroendocrine L cells, indicating it may be a satiety signal. In humans, PYY inhibits food intake and gastrointestinal transit in both lean and obese subjects.

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)

Urocortin III is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin II , frog sauvagine, and piscine urotensin I.1 Human urocortin III shares 90, 40, 37, and 21% identity to mouse urocortin III , mouse urocortin II , human urocortin , and mouse urocortin, respectively. Urocortin III selectively binds to type 2 CRF receptors (Kis = 21.7, 13.5, and >100 nM for rat CRF2α, rat CRF2β, and human CRF1, respectively). It stimulates cAMP production in CHO cells expressing rat CRF2α and mouse CRF2β (EC50s = 0.16 and 0.12 nM, respectively) as well as cultured anterior pituitary cells expressing endogenous CRF2β. Urocortin III is co-released with insulin to potentiate glucose-stimulated somatostatin release in vitro in human pancreatic β-cells.2 In vivo, urocortin III reduces food intake in a dose- and time-dependent manner in mice with a minimum effective dose (MED) of 0.3 nmol/animal.3 It increases swimming time in a forced swim test in mice, indicating antidepressant-like activity.4References1. Lewis, K., Li, C., Perrin, M.H., et al. Identification of urocortin III, an additional member of the corticotropin-releasing factor (CRF) family with high affinity for the CRF2 receptor. Proc. Natl. Acad. Sci. U.S.A. 98(13), 7570-7575 (2001).2. van der Meulen, T., Donaldson, C.J., Cáceres, E., et al. Urocortin3 mediates somatostatin-dependent negative feedback control of insulin secretion. Nat. Med. 21(7), 769-776 (2015).3. Pelleymounter, M.A., Joppa, M., Ling, N., et al. Behavioral and neuroendocrine effects of the selective CRF2 receptor agonists urocortin II and urocortin III. Peptides 25(4), 659-666 (2004).4. Tanaka, M., Kádár, K., Tóth, G., et al. Antidepressant-like effects of urocortin 3 fragments. Brain Res. Bull. 84(6), 414-418 (2011). Urocortin III is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin II , frog sauvagine, and piscine urotensin I.1 Human urocortin III shares 90, 40, 37, and 21% identity to mouse urocortin III , mouse urocortin II , human urocortin , and mouse urocortin, respectively. Urocortin III selectively binds to type 2 CRF receptors (Kis = 21.7, 13.5, and >100 nM for rat CRF2α, rat CRF2β, and human CRF1, respectively). It stimulates cAMP production in CHO cells expressing rat CRF2α and mouse CRF2β (EC50s = 0.16 and 0.12 nM, respectively) as well as cultured anterior pituitary cells expressing endogenous CRF2β. Urocortin III is co-released with insulin to potentiate glucose-stimulated somatostatin release in vitro in human pancreatic β-cells.2 In vivo, urocortin III reduces food intake in a dose- and time-dependent manner in mice with a minimum effective dose (MED) of 0.3 nmol/animal.3 It increases swimming time in a forced swim test in mice, indicating antidepressant-like activity.4 References1. Lewis, K., Li, C., Perrin, M.H., et al. Identification of urocortin III, an additional member of the corticotropin-releasing factor (CRF) family with high affinity for the CRF2 receptor. Proc. Natl. Acad. Sci. U.S.A. 98(13), 7570-7575 (2001).2. van der Meulen, T., Donaldson, C.J., Cáceres, E., et al. Urocortin3 mediates somatostatin-dependent negative feedback control of insulin secretion. Nat. Med. 21(7), 769-776 (2015).3. Pelleymounter, M.A., Joppa, M., Ling, N., et al. Behavioral and neuroendocrine effects of the selective CRF2 receptor agonists urocortin II and urocortin III. Peptides 25(4), 659-666 (2004).4. Tanaka, M., Kádár, K., Tóth, G., et al. Antidepressant-like effects of urocortin 3 fragments. Brain Res. Bull. 84(6), 414-418 (2011).

Urocortin II is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin III , frog sauvagine, and piscine urotensin I.1 Mouse urocortin II shares 34 and 42% sequence homology with rat CRF and urocortin . It is expressed in mouse paraventricular, supraoptic, and arcuate nuclei of the hypothalamus, the locus coeruleus, and in motor nuclei of the brainstem and spinal ventral horn. Urocortin II selectively binds to CRF1 over CRF2 receptors (Kis = 0.66 and >100 nM, respectively) and induces cAMP production in CHO cells expressing CRF2 (EC50 = 0.14 nM). In vivo, urocortin II suppresses nighttime food intake by 35% in rats when administered intracerebroventricularly at a dose of 1 μg. Urocortin II (0.1 and 0.5 μg, i.c.v) stimulates fecal pellet output, increases distal colonic transit, and inhibits gastric emptying in mice.2References1. Reyes, T.M., Lewis, K., Perrin, M.H., et al. Urocortin II: A member of the corticotropin-releasing factor (CRF) neuropeptide family that is selectively bound by type 2 CRF receptors. Proc. Natl. Acad. Sci. U.S.A. 98(5), 2843-2848 (2001).2. Martinez, V., Wang, L., Million, M., et al. Urocortins and the regulation of gastrointestinal motor function and visceral pain. Peptides 25(10), 1733-1744 (2004). Urocortin II is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin III , frog sauvagine, and piscine urotensin I.1 Mouse urocortin II shares 34 and 42% sequence homology with rat CRF and urocortin . It is expressed in mouse paraventricular, supraoptic, and arcuate nuclei of the hypothalamus, the locus coeruleus, and in motor nuclei of the brainstem and spinal ventral horn. Urocortin II selectively binds to CRF1 over CRF2 receptors (Kis = 0.66 and >100 nM, respectively) and induces cAMP production in CHO cells expressing CRF2 (EC50 = 0.14 nM). In vivo, urocortin II suppresses nighttime food intake by 35% in rats when administered intracerebroventricularly at a dose of 1 μg. Urocortin II (0.1 and 0.5 μg, i.c.v) stimulates fecal pellet output, increases distal colonic transit, and inhibits gastric emptying in mice.2 References1. Reyes, T.M., Lewis, K., Perrin, M.H., et al. Urocortin II: A member of the corticotropin-releasing factor (CRF) neuropeptide family that is selectively bound by type 2 CRF receptors. Proc. Natl. Acad. Sci. U.S.A. 98(5), 2843-2848 (2001).2. Martinez, V., Wang, L., Million, M., et al. Urocortins and the regulation of gastrointestinal motor function and visceral pain. Peptides 25(10), 1733-1744 (2004).

HS024 是一种选择性的MC4受体拮抗剂，对 MC4、MC5、MC3 和 MC1 的Ki 分别为 0.29、3.29、5.45 和 18.6 nM。HS024 增加食物摄入。

HS014 TFA 是一种高效、选择性的黑素皮质素-4(MC4)受体拮抗剂，对人 MC4、MC1、MC3 和 MC5 受体的Ki 值分别为 3.16、108、54.4 和 694 nM。HS014 TFA 增加自由喂养大鼠的食物摄取量。

Obestatin(rat) TFA 是一个包含23个氨基酸的肽，由Ghrelin基因编码。该化合物能够抑制食欲和空肠收缩，并能减缓体重增加。同时，Obestatin(rat) TFA 作为G 蛋白偶联受体 39 (GPR39) 的内源性配体，发挥抗炎、抗心肌梗塞和抗氧化功能。

[D-Trp34]-Neuropeptide Y TFA，一种高效且选择性的神经肽Y (NPY) Y5受体激动剂，其在NPY Y1、Y2、Y4及Y6受体上的活性显著低于Y5受体。该化合物能显著提高大鼠的食物摄入量。

[Leu31,Pro34]-Neuropeptide Y(human,rat) TFA 是一种针对神经肽 YY1受体的特定激动剂，并亦能够激活Y4和Y5受体。该化合物能提高麻醉大鼠的血压并增加食物摄入。

[cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic Polypeptide 为高效且选择性的神经肽 YY5 受体激动剂，其与 hY5 受体的结合 IC50 值为 0.24 nM，已知可促进饮食摄入。

Orexin B, rat, mouse (Rat orexin B) TFA，作为一种内源性促进食欲的(Orexin receptor)激动剂，通过结合并激活两个亲密相关的孤儿G蛋白偶联受体OX1-R和OX2-R，促进食物摄入和能量消耗，并在睡眠-觉醒调节中扮演关键角色。

Melanin Concentrating Hormone, salmon TFA (MCH (salmon) TFA) 是在硬骨鱼的垂体中发现的 19 个氨基酸组成的神经肽，它调节食物摄入，能量平衡，睡眠状态和心血管系统。Melanin Concentrating Hormone, salmon TFA (MCH (salmon) TFA) 是 SLC-1/GPR24和 MCHR2的配体。

Peptide YY (pig) 是一种由36个氨基酸组成的胃肠肽，源自猪的十二指肠。该化合物通过激活Y2 receptor来降低食欲和食物摄入量，主要在胰腺的内分泌细胞中发现，对肠动力和心血管系统具有重要影响。

Stresscopin-related peptide (human) 是 2 型 CRH 受体的特异性配体。Stresscopin-related peptide (human) 抑制食物摄入，延迟胃排空，并减少热引起的水肿。Stresscopin-related peptide (human) 在应激后维持体内平衡，可用于应激相关疾病的研究。

Cagrilintide是一种长效的胰淀素（amylin）类似物，是胰淀素受体和降钙素(Calcitonin)受体的双重激动剂，能够降低体重并减少食物摄入，可用于研究肥胖。

Beinaglutide 是一种重组人 GLP-1(rhGLP-1) 多肽，与人 GLP-1(7-36) 具有几乎 100% 的同源性。Beinaglutide 在血糖控制、抑制食物摄入和胃排空和促进体重减轻方面表现出依赖于剂量的作用。Beinaglutide 具有研究超重/肥胖和非酒精性脂肪性肝炎 (NASH) 的潜力。

Agouti-related Protein (AGRP) (83-132) Amide (human)，一种AGRP的片段，主要在下丘脑弓状核中表达。该化合物主要通过作为黑皮质素-4受体(MC4R)的反向激动剂来增加食物摄入。