hypothalamus

JNJ-31020028是神经肽Y2受体选择性可脑渗透抑制剂，对人Y2和鼠源Y2受体pIC50值分别为8.07和8.22，其神经肽 Y2 受体的选择性比人 Y1 Y4 Y5 受体高 100 倍。

Galantide acetate 是一种特殊的甘丙肽受体 (galanin receptor) 拮抗剂，是一种由甘丙肽和 P 物质片段组成的肽段，在大鼠下丘脑可识别两类甘丙肽结合位点 (KD 分别小于 0.1 nM 和 ~6 nM)。Galantide 剂量依赖性 (IC50=1.0 nM) 拮抗甘丙肽介导的葡萄糖诱导的小鼠胰岛胰岛素分泌抑制。Galantide acetate 似乎与单一的 SP 受体群结合 (KD~40 nM)。

β-Endorphin (1-27) (human) acetate 存在于大脑垂体和下丘脑中，具有镇痛活性。 β-Endorphin (1-27) (human) acetate 是一种阿片受体激动剂，对 μ-阿片受体和 δ-阿片受体具有较好的亲和力。

Vasopressin acetate 是一种环状九肽，在下丘脑中枢合成。 Vasopressin acetate 作为一种神经递质，通过与特定的 G 蛋白偶联受体结合发挥其作用。

Melanin Concentrating Hormone, salmon acetate (MCH (salmon))(87218-84-6 free base) 是一种 19 个氨基酸的环状肽，主要在下丘脑中表达。

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。

β-Endorphin, human, a prominent endogenous peptide found in the hypophysis cerebri and hypothalamus, is an agonist of [opioid receptor].

Pregnant mare serum gonadotropin (PMSG) 是用于促进动物卵泡发育及排卵的促性腺激素。该激素可通过激活体内的血液激素、促性腺激素以及前脑垂体和下丘脑中的细胞质雌二醇受体，调节相关生理过程。在畜牧业中，Pregnant mare serum gonadotropin 用以增加繁殖效率；此外，它也被应用于研究发情周期的调节。

Vasopressin-d5 TFA为Vasopressin-d5的TFA盐形式，并作为Vasopressin的同位素标记物。Vasopressin本身是一种在下丘脑中部合成的环状九肽。它参与下丘脑-垂体-肾上腺轴中的功能，通过加强对促皮质素释放因子的刺激，从而调控垂体的促皮质素分泌。此外，Vasopressin还能作为神经递质，通过与特定的G蛋白偶联受体相结合来发挥作用。

Bam 12P acetate 是牛肾上腺、垂体和下丘脑中推定的脑啡肽前体。

Dynorphin (1-8) is an opioid octapeptide from the porcine hypothalamus. It comprises the N-terminal eight residues of dynorphin.

Proxyfan(Proxifan)是一种高亲和力的组胺H3受体的protean拮抗剂 激动剂，具有从完全激动剂到完全逆激动剂的全谱药理活性，取决于给定组织或脑区域内组成活性和静止H3受体之间的竞争。Proxyfan在喂食相关的下丘脑腹内侧核中作为中性拮抗剂，在大鼠基底外侧杏仁核（BLA）中作为激动剂。

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.

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).

Alaproclate is a selective serotonin reuptake inhibitor (SSRI).1,2 It inhibits depletion of serotonin (5-HT) induced by 4-methyl-α-ethyl-m-tyramine in rat cerebral cortex, hippocampus, hypothalamus, and striatum (EC50s = 18, 4, 8, and 12 mg kg, respectively).1 Alaproclate inhibits NMDA-evoked currents and depolarization-induced voltage-dependent potassium currents in rat hippocampal neurons (IC50s = 1.1 and 6.9 μM, respectively) and does not inhibit GABA-evoked currents when used at concentrations up to 100 μM.2 It increases sirtuin 1 (SIRT1) levels in N2a murine neuroblastoma cells expressing apolipoprotein E4 (ApoE4; IC50 = 2.3 μM) and in the hippocampus in the FXFAD-ApoE4 transgenic mouse model of Alzheimer's disease when administered at a dose of 20 mg kg twice daily.3 Alaproclate (40 mg kg) decreases immobility time in the forced swim test in rats, indicating antidepressant-like activity.4References1. Michael, G.B., Eidam, C., Kadlec, K., et al. Increased MICs of gamithromycin and tildipirosin in the presence of the genes erm(42) and msr(E)-mph(E) for bovine Pasteurella multocida and Mannheimia haemolytica. Journal of Antimicrobial Chemotherapy 67(6), 1555-1557 (2012).2. Svensson, B.E., Werkman, T.R., and Rogawski, M.A. Alaproclate effects on voltage-dependent K+ channels and NMDA receptors: Studies in cultured rat hippocampal neurons and fibroblast cells transformed with Kv1.2 K+ channel cDNA. Neuropharmacology 33(6), 795-804 (1994).3. Campagna, J., Soilman, P., Jagodzinska, B., et al. A small molecule ApoE4-targeted therapeutic candidate that normalizes sirtuin 1 levels and improves cognition in an Alzheimer's disease mouse model. Sci. Rep. 8(1), 17574 (2018).4. Danysz, W.P., A., Kostowski, W., Malatynska, E., et al. Comparison of desipramine, amitriptyline, zimeldine and alaproclate in six animal models used to investigate antidepressant drugs. Pharmacol. Toxicol. 62(1), 42-50 (1988). Alaproclate is a selective serotonin reuptake inhibitor (SSRI).1,2 It inhibits depletion of serotonin (5-HT) induced by 4-methyl-α-ethyl-m-tyramine in rat cerebral cortex, hippocampus, hypothalamus, and striatum (EC50s = 18, 4, 8, and 12 mg kg, respectively).1 Alaproclate inhibits NMDA-evoked currents and depolarization-induced voltage-dependent potassium currents in rat hippocampal neurons (IC50s = 1.1 and 6.9 μM, respectively) and does not inhibit GABA-evoked currents when used at concentrations up to 100 μM.2 It increases sirtuin 1 (SIRT1) levels in N2a murine neuroblastoma cells expressing apolipoprotein E4 (ApoE4; IC50 = 2.3 μM) and in the hippocampus in the FXFAD-ApoE4 transgenic mouse model of Alzheimer's disease when administered at a dose of 20 mg kg twice daily.3 Alaproclate (40 mg kg) decreases immobility time in the forced swim test in rats, indicating antidepressant-like activity.4 References1. Michael, G.B., Eidam, C., Kadlec, K., et al. Increased MICs of gamithromycin and tildipirosin in the presence of the genes erm(42) and msr(E)-mph(E) for bovine Pasteurella multocida and Mannheimia haemolytica. Journal of Antimicrobial Chemotherapy 67(6), 1555-1557 (2012).2. Svensson, B.E., Werkman, T.R., and Rogawski, M.A. Alaproclate effects on voltage-dependent K+ channels and NMDA receptors: Studies in cultured rat hippocampal neurons and fibroblast cells transformed with Kv1.2 K+ channel cDNA. Neuropharmacology 33(6), 795-804 (1994).3. Campagna, J., Soilman, P., Jagodzinska, B., et al. A small molecule ApoE4-targeted therapeutic candidate that normalizes sirtuin 1 levels and improves cognition in an Alzheimer's disease mouse model. Sci. Rep. 8(1), 17574 (2018).4. Danysz, W.P., A., Kostowski, W., Malatynska, E., et al. Comparison of desipramine, amitriptyline, zimeldine and alaproclate in six animal models used to investigate antidepressant drugs. Pharmacol. Toxicol. 62(1), 42-50 (1988).

PACAP-related peptide (PRP) is an endogenous 29-amino acid peptide that belongs to the secretin/glucagon superfamily of peptides, which includes secretin , glucagon , glucagon-like peptide-1 , GLP-2 , and pituitary adenylate cyclase-activating polypeptide . It is expressed in rat hypothalamus as well as within the nerves of the median eminence, the anterior pituitary, bed nucleus of the stria terminalis, cerebellum, cerebral cortex, and amygdala. PRP is also expressed in vaginal, uterine cervical, uterine horn, fallopian tube, and ovarian tissues from the rat female genital tract and is present in extracts of male testis tissue.

Cyclic ADP-ribose (cADP-ribose) is an endogenous metabolite of NAD+ that mobilizes the release of stored Ca2+ in the endoplasmic reticulum via ryanodine receptors in various cell types.[1],[2],[3],[4],[5] This second messenger is generated via the cADP-ribose synthases CD38 and CD157.[6],[5],[7] cADP-Ribose may also trigger the cell surface Ca2+ influx channel TRPM2 in a temperature-dependent manner.[8] In vitro, cADP-ribose modulates Ca2+ signaling in rat and mouse cardiomyocytes treated with isoproterenol , and treatment with this metabolite at 100 μM under heat stress conditions induces the release of oxytocin from the mouse hypothalamus.[9],[4]

Acetyl β-endorphin (1-26) is a neuropeptide found in rat hippocampus, brain stem, and pituitary. It is also present in the human hypothalamus, where it comprises approximately 4.9% of total β-endorphin peptides. Acetyl β-endorphin (1-26) is produced through posttranslational processing of β-endorphin and is processed similarly in rat and human hypothalamus. Levels of acetyl β-endorphin (1-26) increase in the rat pars intermedia and brain stem following chronic administration of haloperidol .

Nafarelin is a gonadotropin-releasing hormone agonist (GnRH agonist) which acts as an analog of GnRH. Nafarelin increases the release of FSH and LH by the anterior pituitary, which in turn leads to an increase of estrogen progesterone. When administered, Nafarelin has the purpose of causing increase estrogen that will negatively feed back upon hypothalamus to decrease GnRH ( negative feedback loop ) Through negative feedback, Nafarelin causes a decrease in pituitary secretion of gonadotropins luteinizing hormone (LH) and follicle stimulating hormone (FSH). Nafarelin may be used in the treatment of estrogen-dependent conditions (such as endometriosis or uterine fibroids), to treat central precocious puberty, and to control ovarian stimulation in IVF. It is normally delivered via a nasal spray. Nafarelin acetate is marketed by Searle (now part of Pfizer) under the brand name Synarel.

Cinnarizine clofibrate is a calcium channel protein inhibitor as well as an antihistamine channel blocker. The compound is a drug derivative of piperazine. Cinnarizine is used for the control of vomiting due to motion sickness. It acts by interfering with the signal transmission between vestibular apparatus of the inner ear and the vomiting centre of the hypothalamus

TAK-683 acetate是一种高效的KISS1R激动剂(IC50=170 pM)，改善了代谢稳定性。作为九肽metastin的类似物，对人和大鼠的EC50值分别为0.96 nM和1.6 nM。该化合物通过消耗下丘脑GnRH，能够降低血浆FSH、LH、睾酮水平，展示了对研究激素依赖性前列腺癌的潜力。

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。

LH-RH II (chicken) 为家鸡下丘脑黄体生成素释放激素(LHRH)两种形式之一，亦为哺乳动物LHRH的结构变体。该化合物促进家鸡促性腺激素释放。

LH-RH (7-10)，一种由性腺激素释放激素 (LHRH) 在垂体和下丘脑降解过程中形成的主要四肽降解产物之一，存在于巨噬细胞、I 型样及II 型肺细胞中。