at-2 receptor

CGP-42112 acetate是一种有效的血管紧张素受体 AT2 激动剂,抑制 LPS 产生的蛋白激酶 A 活性的增加。

CL-329167, a angiotensin type 1 receptor antagonist, is used potentially for the treatment of hypertension.

1-Aminocyclopropane-1-carboxylic acid (ACC) 是内源性代谢产物的一种。

Siramesine (Lu 28-179) 是sigma-2受体激动剂，通过线粒体的不稳定溶酶体触发细胞死亡，有强大的抗癌活性。它对 sigma-2 受体具有亚纳摩尔亲和力，IC50为 0.12 nM。它对 sigma-2 受体的选择性是 sigma-1 受体的 140倍，IC50为 17 nM。

2-Furoyl-LIGRLO-amide TFA is a peptide that acts as a proteinase-activated receptor-2 (PAR2) agonist, and contains a furoyl group addition at its N-terminal.

GW842166X 是一种选择性 cannabinoid receptor 2 激活剂，IC50=63 nM。

BP 897 (2-Naphthalenecarboxamide, N-[4-[4-(2-methoxyphenyl)-1-piperazinyl]butyl]-) 是一种有效的部分多巴胺D3受体激动剂和弱D2受体拮抗剂，在多巴胺 D3 受体(Ki=0.92 nM) 上显示出高亲和力，而在 D2 受体上显示出 70 倍的低亲和力 (Ki=61 nM)。它表现出对可卡因寻求行为的选择性抑制。

Spexin acetate(1370290-58-6 free base) 是一种有效的甘丙肽受体 2 3 (GAL2 GAL3) 激动剂（EC50 值分别为 45.7 和 112.2 nM）。对甘丙肽受体 1 没有显着的活性。抑制脂肪细胞对长链脂肪酸的摄取并减少饮食诱导的肥胖小鼠和大鼠的食物消耗。减少金鱼的 LH 分泌。在体内表现出抗焦虑作用。

3-(2-aminopropyl)phenol hydrochloride 是一种用作分子结构单元的苯乙胺类化合物。它是一种精神活性药物，是5-HT1A、5-HT1B 和5-HT2C 等几种血清素受体的部分激动剂，也是5-HT2A 受体的拮抗剂。

2-(5,7-dichloro-1H-indol-3-yl)ethan-1-amine 是一种吲哚胺类化合物，在结构上与血清素相似。它是5-HT2A 受体的选择性激动剂，在神经科学领域具有潜在的应用。

NS11394 是可口服GABAA 的阳性变构调节剂 (PAM)，Ki 值为 0.5 nM。它对GABAA 的选择性依次为 α5、α3、α2 和α1 受体，具有抗炎和抗焦虑活性。

COR659 是一种有效的 GABAB 的阳性变构调节剂。COR659具有缓解大鼠对酒精和巧克力成瘾的作用。

Unifiram 是一种认知增强剂。 Unifiram 诱导大鼠海马 CA1 区场兴奋性突触后电位 (fEPSP) 幅度的持久增加 (EC50= 27 nM) 并增加大鼠大脑皮层中乙酰胆碱 (ACh) 的释放。

Bavisant dihydrochloride hydrate (JNJ31001074AAC) is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD. in vivo: Mean change

1,2,3,6,7,8-六氯二苯并-p-二噁英是一种多氯代二苯并二噁英（PCDD）。它是芳香烃受体（AhR; EC50s分别为5.4和9.3 nM，在4和8小时的报告检测中）的激动剂。1,2,3,6,7,8-六氯二苯并-p-二噁英（0.5和2 µg kg）降低了小鼠对羊红血球的抗体产生。在动物饲料和靠近市政废物焚烧炉的空气中均有发现。

Tat-M2NX是一种瞬时受体电位麦拉斯汀2（TRPM2）的肽类拮抗剂。在25到100µM的浓度范围内，能够抑制表达人类TRPM2的HEK293细胞中氢过氧化物诱导的钙离子流入。在体内，Tat-M2NX（20 mg/kg）通过在中大脑动脉阻塞（MCAO）诱导的中风模型中，如果在阻塞前或阻塞后3小时内给药，能减少雄性小鼠的脑梗塞体积，但对雌性小鼠无效。

Tat-CBD3是一种抑制N型电压门控钙通道Cav2.2与collapsin response mediator protein 2 (CRMP2)之间的蛋白质-蛋白质相互作用的抑制剂。它还能抑制CRMP2与NMDA受体NR2B亚单位之间的蛋白质-蛋白质相互作用。在无细胞实验中，Tat-CBD3 (10 µM)能将Cav2.2-CRMP2相互作用抑制43%，并在免疫共沉淀实验中抑制NMDA受体NR2B亚单位-CRMP2相互作用。它能在初级大鼠背根神经节 (DRG) 神经元中减少约60%的电压诱导钙电流，并在初级大鼠海马神经元中减少谷氨酸诱导的胞内钙水平增加。Tat-CBD3 (20 mg/kg)在大鼠中脑动脉闭塞 (MCAO) 引发的脑缺血模型中减少梗死体积。鞘内给药Tat-CBD3 (20 µg/5 µl)可防止大鼠卡拉胶诱导的热敏感性。

S1PL-IN-31是一种鞘氨醇-1-磷酸(S1P)裂解酶的抑制剂(IC50 = 210 nM)，同时也是Smoothened(Smo)受体的对抗剂(IC50 = 440 nM)。在体内，S1PL-IN-31 (每天2 mg kg)能够防止实验性自身免疫性脑炎(EAE)模型大鼠中，由髓鞘少突胶质细胞糖蛋白(MOG)肽段MOG29-152诱发的颈部及胸部淋巴细胞渗透和神经肌肉虚弱。该化合物降低了大鼠的淋巴细胞总数及CD4+ T细胞、CD8+ T细胞和B细胞的水平。S1PL-IN-31 (每天3及10 mg kg剂量)在雄性和雌性大鼠心脏和淋巴结中增加了S1P水平，并且在雌性大鼠中降低了心率。

Prostaglandin H2 (PGH2), initially isolated from the incubation of arachidonic acid with ovine seminal vesicle microsomes, acts as a potent vasoconstrictor. It serves as the precursor for all 2-series prostaglandins (PGs) and thromboxanes (TXs). Moreover, as a TP receptor agonist, PGH2 irreversibly aggregates human platelets at concentrations of 50-100 ng ml.

19(R)-Hydroxylated prostaglandins (PGs) are present at µg ml concentrations in the semen of some mammalian species, notably primates, with the majority being from the PGE series and featuring a 15(S),19(R) hydroxyl stereochemistry. These compounds are also observed in marsupials' seminal plasma, where F-type 1 and 2-series compounds are predominant. The 15(R)-hydroxy epimer represents the inverse or unnatural isomer at C-15 for these 19-hydroxylated PGs. Although the biological function of 19(R)-hydroxylated PGs remains unclear, 19(R)-hydroxylation in the F-series leads to a notable reduction in receptor-mediated biological activity in certain assays.

ZLY032 is a dual agonist of free fatty acid receptor 1 (FFAR1 GPR40; EC50= 68 nM in a FLIPR assay) and peroxisome proliferator-activated receptor δ (PPARδ; EC50= 102 nM in a reporter assay).1It is selective for FFAR1 and PPARδ over PPARα and PPARγ (EC50s = >10 μM for both). ZLY032 (40 mg kg, twice per day) reduces blood glucose levels in an oral glucose tolerance test and decreases plasma total cholesterol and triglyceride levels in theob obmouse model of metabolic disease.2It reduces hepatic steatosis and plasma alanine transaminase (ALT) and aspartate aminotransferase (AST) levels in a mouse model of non-alcoholic steatohepatitis (NASH) induced by a methionine and choline-deficient diet at the same dose. 1.Li, Z., Chen, Y., Zhou, Z., et al.Discovery of first-in-class thiazole-based dual FFA1 PPARδ agonists as potential anti-diabetic agentsEur. J. Med. Chem.164352-365(2019) 2.Li, Z., Zhou, Z., Hu, L., et al.ZLY032, the first-in-class dual FFA1 PPARδ agonist, improves glucolipid metabolism and alleviates hepatic fibrosisPharmacol Res.159105035(2020)

Prostaglandin F1α (PGF1α) is the putative metabolite of dihomo-γ-linolenic acid (DGLA) via the cyclooxygenase (COX) pathway. Both PGF1α and PGF2α have been shown to act as priming pheromones for male Atlantic salmon with a threshold concentration of 10-11 M. [1] PGF1α binds to the ovine corpus luteum FP receptor at only 8% of the relative potency of PGF2α. [2] It is only half as active as PGF2α in inducing human respiratory smooth muscle contractions in vitro. [3]

Rp-2'-Deoxyuridine-5'-O-(1-thiotriphosphate) (Rp-dUTP-α-S) 是含硫核苷酸 dUTP-α-S 的同分异构体，也是嘌呤P2Y2受体的激动剂。在表达P2Y2受体的1321N1星形胶质瘤细胞中，该化合物特异性诱导肌醇磷酸积累（EC50 = 12.5 µM），相较于表达P2Y4的1321N1细胞，在10 µM浓度下效果更显著。

9(Z),11(E)-Conjugated linoleic acid is an isomer of linoleic acid that has been found in beef and milk fat.1It binds to peroxisome proliferator-activated receptor α (PPARα; IC50= 140 nM) and activates the receptor in a reporter assay using COS-1 cells expressing mouse PPARα when used at a concentration of 100 μM.29(Z),11(E)-Conjugated linoleic acid inhibits TNF-α-inducedGLUT4expression and increases insulin-stimulated glucose transport in 3T3-L1 adipocytes.3Dietary administration of 9(Z)11(E)-conjugated linoleic acid reduces serum fasting glucose, insulin, and triglyceride levels and decreases white adipose tissue macrophage infiltration inob obmice. It also increases body weight gain and body fat in weanling mice.4[Matreya, LLC. Catalog No. 1278] 1.Shultz, T.D., Chew, B.P., Seaman, W.R., et al.Inhibitory effect of conjugated dienoic derivatives of linoleic acid and β-carotene on the in vitro growth of human cancer cellsCancer Lett.63(2)125-133(1992) 2.Moya-Camarena, S.Y., Heuvel, J.P.V., Blanchard, S.G., et al.Conjugated linoleic acid is a potent naturally occurring ligand and activator of PPARαJ. Lipid Res.40(8)1426-1433(1999) 3.Moloney, F., Toomey, S., Noone, E., et al.Antidiabetic effects of cis-9, trans-11-conjugated linoleic acid may be mediated via anti-inflammatory effects in white adipose tissueDiabetes56(3)574-582(2007) 4.Pariza, M.W., Park, Y., and Cook, M.E.The biologically active isomers of conjugated linoleic acidProg. Lipid Res.40(4)283-298(2001)