kappa opioid receptor

ZT 52656A hydrochloride 是一种 kappa 阿片样物质的选择性激动剂，用于预防或减轻眼部疼痛。

LY2444296 (FP3FBZ) 是 kappa opioid receptor (Ki = 1 nM) 的具有口服活性的和选择性拮抗剂。

Difelikefalin acetate (CR 845 acetate) 是一种外周受限的 kappa 阿片受体激动剂。CR845 表现出低 P450 CYP 抑制和对大脑的低渗透性。

DuP 747 HCl 是一种选择性 kappa 激动剂，具有镇痛活性。DuP 747 由两种构型组成。

Matrine (Vegard) 是一种从槐属植物中分离出来的生物碱，可作为一种κ阿片受体激动剂，有抗肿瘤活性。

Dup 747 is an analgesic that binds with high affinity and selectivity to the kappa-opioid receptor.

JDTic Dihydrochloride是一种高亲和力和选择性的κ-opioid receptor(KOR)拮抗剂，能够阻断dynorphin-KOR信号，具有抗抑郁、抗焦虑及抑制可卡因与尼古丁复吸的作用。

RB-64 (22-Thiocyanatosalvinorin A)为一种kappa-opioid receptor选择性激动剂，展现出高效性，其EC50值仅为0.077 nM。

5'-Guanidinonaltrindole (GNTI) 为一种选择性 kappa opioid receptor 拮抗剂。

KOR agonist 4 (compound 39) 是 κ 阿片受体 (Kappa Opioid Receptor) 的激动剂，并且是 G 蛋白信号传导的激活剂。它与 GTPγS 结合的EC50 为 14 nM，Emax为 83%。在人肝细胞中，其表现出中等至高的内在清除率。相比 μ (MOR) 和 δ (DOR) 阿片受体，KOR agonist 4 对 κ (KOR) 阿片受体的选择性分别高出 60 倍和 810 倍。该化合物适用于中枢神经系统 (CNS) 疾病的研究。

PIPE-3297 (compound 25) 是一种选择性的 kappa 阿片受体 (KOR) 激动剂，能够激活 G 蛋白信号通路，EC50为 1.1 nM，同时表现出低 β-arrestin-2 招募活性 (10%)。此外，PIPE-3297 能够诱导髓鞘形成，并具备抗炎特性。

CJ-15208 is a potent and selective κ-opioid receptor antagonist from a fungus, Ctenomyces serratus ATCC15502 (IC50 are 47 nM for kappa, 260 nM for mu, and 2,600 nM for delta respectly). In the electrically-stimulated twitch response assay of rabbit vas de

LY255582 是一种具有选择性的中枢活性阿片受体拮抗剂，对 mu、delta 和 kappa 受体具有高亲和力 ，Ki 分别为 0.4 nM、5.2、2.0 nM。LY255582 可以抑制饮食相关的中脑边缘多巴胺水平的增加，并减少食物摄入的消耗。LY255582 常用于对肥胖的研究。LY255582是用于阿片受体介导的细胞信号传导研究的潜在化合物。

MR2034 is an agonist of kappa-Opioid receptor. MR2034 stimulates hypothalamic-pituitary-adrenal axis.

R-84760 is a κ-opioid receptor agonist. R-84760 produces an extremely potent antinociceptive effect against tonic pain through the kappa-opioid receptors; the sites of action of subcutaneously administered R-84760 are the supraspinal and spinal loci in th

U-54494A hydrochloride 是一种与 κ 阿片受体激动剂相关的苯甲酰胺衍生物，U-54494A hydrochloride 具有抗惊厥活性。

Selective sigma (σ) receptor ligand. Displays high affinity for σ1; also binds at σ2 sites (Ki = 1.5 nM and 50.8 nM respectively). Selective over a range of receptor types including dopaminergic and muscarinic receptors, DAT and SERT. Prezzavento et al (2007) Novel sigma receptor ligands: synthesis and biological profile. J.Med.Chem. 50 951 PMID:17328523 |Prezzavento et al (2008) A new sigma ligand, (±)-PPCC, antagonizes kappa opioid receptor-mediated antinociceptive effect. Life Sci. 82 549 PMID:18261749 |Antonini et al (2009) Anti-amnesic properties of (±)-PPCC, a novel sigma receptor ligand, on cognitive dysfunction induced by selective cholinergic lesion in rats. J.Neurochem. 109 744 PMID:19245662

Difelikefalin (CR-845; FE-202845) is a peripherally restricted, selective agonist of the kappa opioid receptor (KOR). It exhibits anti-inflammatory properties and holds promise for modulating pruritus in conditions associated with chronic kidney disease.

Asimadoline (EMD-61753) 是一种 κ-阿片(κ-opioid)受体激动剂，对豚鼠和人重组 κ-opioid 的IC50值分别为 5.6 和 1.2 nM。它可改善糖尿病大鼠的异常性疼痛，具有外周抗炎作用，并有用于肠易激综合征的研究潜力。

4-Me-PDTic is a potent and selective Kappa Opioid Receptor Antagonist. 4-Me-PDTic had a Ke = 0.37 nM in a [35S]GTPγS binding assay and was 645- and >8100-fold selective for the κ relative to the μ and δ opioid receptors, respectively. Calculated logBB and CNS (central nervous system) multiparameter optimization (MPO) and low molecular weight values all predict that 4-Me-PDTic will penetrate the brain and pharmacokinetic studies in rats shows that 4-Me-PDTic does indeed penetrate the brain.

4-Me-PDTic is a potent and selective kappa opioid receptor antagonist.

GNTI TFA is a selective kappa opioid receptor antagonist.

Riminkefon 是κ 阿片受体的激动剂。

ICI-204879 HCl is a potent and selective agonists at the opioid kappa-receptor.