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。

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。

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。

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.

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。

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.

Enadoline (Free Base) is a kappa-opioid receptor agonist; PD 129290 (CAM 570; CI 977) is the S,S(-)-enantiomer; PD 129289 (CAM 569) is the corresponding R,R(+)-enantiomer. In human studies, it produced visual distortions and feelings of dissociation, reminiscent of the effects of salvinorin A. It was studied as a potential analgesic, but abandoned because of the dose-limiting effects of dysphoria, which could be expected from a κ-opioid agonist. There was mention of its potential in treating comatose head injury or stroke victims, where that type of side effect would be immaterial.

nor-Binaltorphimine dihydrochloride is a long-acting potent and highly selective kappa opioid receptor antagonist.