agonism

SB 258719 是高亲和力的、选择性的5-HT7受体拮抗剂，pKi 为7.5。SB 258719在癌症和神经系统疾病领域有研究价值。

Tirzepatide (LY3298176) Acetate(2023788-19-2 free base) 是一种新分子，能够通过结合葡萄糖依赖性促胰岛素多肽（GIP）和胰高血糖素样肽-1（GLP-1）受体的双重激动作用来控制血糖水平。[3]

OP-3633 is an effective and selective steroidal glucocorticoid receptor (GR) antagonist (IC50: 29 nM). OP-3633 shows low progesterone receptor (PR) agonism and androgen receptor (AR) antagonism. It also has an inhibition of GR transcriptional activity.

Romergoline 是一种新合成的麦角碱衍生物，具有独特的药理作用，在正常动物中表现出完全的多巴胺(DA)拮抗作用，而在“去神经”动物模型中表现出完全的DA 拮抗作用。

STAMBP-IN-1是一种新型选择性去泛素酶 STAM 结合蛋白 (STAMBP) 拮抗剂，可降低 NALP7 蛋白水平并抑制 TLR 激动后 IL-1β 的释放。

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。

NXN-188 是一种一流的、双重作用的小分子化合物，结合了神经型一氧化氮合酶 (nNOS) 抑制和 5-HT 受体激动剂，目前正处于急性偏头痛治疗的开发阶段。

SC-17599 在乙酸诱导的扭体实验和热水尾部抽回试验中显示出剂量依赖性的镇痛效果。此化合物还以剂量依赖和纳曲酮敏感的方式诱导Straub尾反应，与吗啡的效果类似。与吗啡不同的是，高剂量的SC-17599并不影响运动活动。总体而言，SC-17599表现出选择性的μ阿片受体激动作用，其行为效应与吗啡相似，尽管存在一些差异。

Aganodine is a guanidine that activates presynaptic imidazoline receptors. Aganodine inhibits the presynaptic release of norepinephrine through its agonism at imidazoline receptors.

BIO592 is a modulator of RORγt. BIO592 triggers inverse agonism of RORγ.

GSK-7227, a novel class of PPARdelta partial agonists, shows potent partial agonism of the PPARdelta target genes CPT1a and PDK4 in skeletal muscle cells.

(±)-WIN 55,212-2 is a potent aminoalkylindole cannabinoid (CB) receptor agonist with a Ki value of 62.3 and 3.3 nM for human recombinant central cannabinoid (CB1) and peripheral cannabinoid (CB2) receptors, respectively. In contrast, the enantiomer (-)-WIN 55,212-3 acts a partial inverse agonist at CB1 (pIC50 = 5.5) and as a competitive neutral antagonist of CB2, reversing the inverse agonism evoked by SR 144528 (pEC50 = 5.3). (+)-WIN 55,212 (mesylate) is a mixture of the two enantiomers, (+)-WIN 55,212-2 and (-)-WIN 55,212-3.

Fabomotizole hydrochloride (CM346 hydrochloride) 是一种具有抗焦虑和神经保护作用的化合物。

PPARγ phosphorylation inhibitor 1 (Compound 10) 是一种有效的 PPARγ结合剂 (IC50: 24 nM)，具有抗糖尿病效果。PPARγ phosphorylation inhibitor 1 对 CDK5 介导的 PPARγ Ser273 磷酸化表现出抑制作用 (IC50: 160 nM)，且几乎无 PPARγ 激动作用。

SC13 是一种新型的 mitragynine 类似物，具有低效Muopioid receptor 激动作用，具有麻醉作用和较轻的不良反应。

PPARγ agonist 1 是 PPARγ 的有效激动剂，能够高效的激活 hPPARγ ，并不引起完全激动，进而能够避免不良反应。PPARγ agonist 1 对代谢紊乱相关心血管疾病表现出研究潜力。

OL-135 is a CNS penetrant, highly potent and selective reversible inhibitor of FAAH. OL-135 exhibits analgesic pharmacology in various animal models without the motor impairment associated with direct CB1 agonism.

Fabomotizole, also known as Afobazole, Obenoxazine and CM346, is an anxiolytic drug launched in Russia in the early 2000s. It produces anxiolytic and neuroprotective effects without any sedative or muscle relaxant actions. Its mechanism of action remains poorly defined however, with GABAergic, NGF- and BDNF-release-promoting, MT1 receptor agonism, MT3 receptor antagonism, and sigma agonism suggested as potential mechanisms. Fabomotizole was shown to inhibit MAO-A reversibly and there might be also some involvement with serotonin receptors.

Fadolmidine, also known as MPV-2426, is a novel and potent alpha2 -adrenoceptor (alpha2) -AR) agonist developed for spinal analgesia. Fadolmidine displayed high affinity and full agonist efficacy at all three human alpha2-adrenoceptor subtypes (A, B and C) in transfected CHO cells with EC50 values (nM) of 0.4, 4.9 and 0.5, respectively. Fadolmidine inhibited also electrically evoked contractions in rat vas deferens demonstrating the activation of rodent presynaptic alpha2D-adrenoceptors with an EC50 value of 6.4 nM. Moreover, fadolmidine was a full agonist at human alpha1A-adrenoreceptor (EC50 value 22 nM) and alpha1B-adrenoreceptor (EC50 value 3.4 nM) in human LNCaP cells and transfected HEK cells, respectively. Agonism at the alpha1-adrenoceptor was also observed in rat vas deferens preparations although at lower potency (EC50 value 5.6 microM). Fadolmidine demonstrated potent alpha2-adrenoceptor agonist activity also in vivo by inhibiting electrically induced tachycardia i......

PF-04479745, also known as PF-4479745, is a potent and selective 5-HT2C agonist (EC50 = 10 nM). PF-4479745 displayed robust pharmacology in a preclinical canine model of stress urinary incontinence (SUI) and no measurable functional agonism at the key selectivity targets 5-HT2A and 5-HT2B in relevant tissue-based assay systems.

Thrombospondin-1 (1016-1023) (human, bovine, mouse) 是 Thrombospondin-1 (TSP-1) 的一部分，是一种具有 CD47 激动作用的多肽。

D3R MOR antagonist 1 (Compound 114) 为D3R MOR拮抗剂，其对D3R和MOR的Ki值分别为46.5 nM和691 nM。该化合物通过MOR的部分激动作用可能具有镇痛效果，同时通过D3R的拮抗作用有助于降低阿片类药物的滥用风险。

D3R MOR antagonist 2（Compound 121）为一种D3R MOR拮抗剂，其Ki值分别为46.5 nM及691 nM。该化合物通过MOR部分激动作用可产生镇痛效果，并通过D3R拮抗减少阿片类药物的潜在滥用风险。

MOR agonist-2 (Compound 46) 为D3R拮抗剂及MOR激动剂，其Ki值分别为7.26 nM和564 nM。MOR agonist-2潜在以MOR部分激动机制实现镇痛效果，并通过D3R拮抗降低阿片类药物的滥用风险。