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Search Results for " kappa-opioid "

37

抑制剂 & 化合物

5

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T11909	LY2444296 FP3FBZ	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	LY2444296 (FP3FBZ) 是 kappa opioid receptor (Ki = 1 nM) 的具有口服活性的和选择性拮抗剂。
TQ0082	Aticaprant LY-2456302,CERC-501	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	Aticaprant (LY-2456302) 是一种有效的中枢渗透性 kappa-阿片受体拮抗剂，Ki 值为 0.807 nM。
T13414	ZT 52656A hydrochloride	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	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。
T0102	Naloxone hydrochloride 盐酸纳洛酮,Naloxone HCl	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	Naloxone hydrochloride (Naloxone HCl) 是一种特异性、没有激动剂活性的opiate 拮抗剂。它是 mu、delta 和 kappa 阿片受体的竞争性拮抗剂。
TP2501	Difelikefalin acetate Difelikefalin acetate(1024828-77-0 free base),CR 845 acetate,Difelikefalin醋酸盐,FE 202845 acetate	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	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。
T1197	Trimebutine maleate Debridat,Polibutin,马来酸曲美布汀	Calcium Channel; Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Membrane transporter/Ion channel; Metabolism; Neuroscience
	Trimebutine maleate (Polibutin) 是一种外周 μ、δ 和 kappa 阿片受体激动剂，用作治疗慢性和急性腹痛的解痉药物。
T28094	MR2034
	MR2034 is an agonist of kappa-Opioid receptor. MR2034 stimulates hypothalamic-pituitary-adrenal axis.
T34877	Tifluadom KC-5103,KC5103,dl-Tifluadom,KC 5103
	Tifluadom is a type of kappa-opioid benzodiazepine.
T71019	Niravoline
	Niravoline is a kappa-opioid agonist.
T69799	4-Me-PDTic
	4-Me-PDTic is a potent and selective kappa opioid receptor antagonist.
T69886	FE-200041
	FE-200041 is a peripheral efficacious kappa opioid agonist.
T69818	GNTI TFA
	GNTI TFA is a selective kappa opioid receptor antagonist.
T24035	Eptazocine hydrobromide MCV 4169,ST-2121,MCV-4169,sT 2121, l-,l-ST-2121
	Eptazocine hydrobromide is an agonist of the Opioid receptor and is a kappa-Opioid receptor agonist. It is also an Opioid analgesic and an Opioid receptor antagonist.
T73339	Anrikefon HSK21542
	Anrikefon (HSK21542) 为 kappa 阿片受体（kappa opioid receptor）激动剂，具缓解疼痛作用。
T27079	CR-665 Acetate FE200665,CR-665,JNJ-38488502,CR665,FE-200665,JNJ38488502
	CR-665, a kappa-opioid agonist, is used potentially for the treatment of postoperative pain.
T25354	Dup 747 Dup-747,Dup747
	Dup 747 is an analgesic that binds with high affinity and selectivity to the kappa-opioid receptor.
T79848	Icalcaprant	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	Icalcaprant为κ阿片受体拮抗剂。
T71370	ICI-204879 HCl
	ICI-204879 HCl is a potent and selective agonists at the opioid kappa-receptor.
T81938	Leumorphin, human	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	Leumorphin, human 作为一种 kappa 型阿片受体 (κ-opioid receptor) 激动剂，有效抑制了豚鼠回肠肌间神经丛-纵向肌肉制剂的收缩。
T11721L	JDTic dihydrochloride	JAK	Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells
	JDTic is a potent antagonist of kappa-opioid receptors (KOR), blocking the κ-agonist U50, 488-induced antinociception.
T71523	Norbinaltorphimine
	nor-Binaltorphimine dihydrochloride is a long-acting potent and highly selective kappa opioid receptor antagonist.
T69851	Riminkefon
	Riminkefon 是κ 阿片受体的激动剂。
T28313	PD 117302 PD-117302,PD117302
	PD 117302 is a nonpeptide opioid compound. It is a selective kappa-opioid agonist. PD 117302 causes naloxone-reversible locomotor impairment and diuresis. It is an Anti-Arrhythmia Agent, an Anticonvulsants, a Cardiovascular Agent, and a Central Nervous Sy
T73522	CR 665 FE 200665,JNJ 38488502 ; FE 200665,JNJ 38488502
	CR 665 (JNJ 38488502) 是一种外周选择性κ-阿片类激动剂。CR 665可以激活 kappa 阿片受体 EC50值为10.9 nM。CR 665 可用于外周疼痛的研究。
T27027	CJ-15208 CJ15,208,CJ-15,208,CJ 15,208.c[Phe-D-Pro-Phe-Trp]
	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
T38419	Difelikefalin CR-845,FE-202845
	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.
T36372	U-54494A hydrochloride
	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。
T28495	R-84760 hydrochloride R84760,R 84760,R 86436,R-86436,R86436
	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
T76631	(N-Me-Tyr1,N-Me-Arg7,D-Leu-NHEt8)-Dynorphin A (1-8)
	(N-Me-Tyr1,N-Me-Arg7,D-Leu-NHEt8)-Dynorphin A (1-8) (E-2078) 是一种稳定的 Dynorphin A (1-8) 类似物，是 kappa 阿片受体 (KOR) 激动剂。
T75916	Dynorphin A TFA
	Dynorphin A TFA, 作为一种内源性阿片肽，主要在中枢神经系统（CNS）中发挥抑制性神经传导的作用。该化合物不仅是kappa阿片受体（KOR）的高效激动剂，还能激活其他阿片受体，包括mu（MOR）和delta（DOR）。Dynorphin A TFA具有诱导神经元死亡的能力，因此在神经系统疾病的研究中具有应用价值。
T27934	LY255582 LY-255582,LY 255582	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	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。
T72423	Endomorphin 1 acetate
	Endomorphin 1 acetate，一种高度选择性的，高亲和力的μ-opioid 受体激动剂 (Ki: 1.11 nM)，对 kappa3结合位点具有高亲和力，Ki 值为 20 到 30 nM 之间。Endomorphin 1 acetate 具有镇痛特性。
T71491	Enadoline (Free Base)
	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 com...
T69798	4-Me-PDTic HCl
	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.
T4633	Asimadoline EMD-61753,阿西马朵林	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	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。
T80421	CSD-CH2(1,8)-NH2	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	CSD-CH2(1,8)-NH2 是一种针对KOR的选择性且竞争性拮抗剂，具有较低的Ki值（6.8 nM），能够抑制DRG神经元内的钙动员，并能拮抗U50,488的抗伤害效应，常用于神经精神疾病研究领域。
T37013	(+/-)-PPCC oxalate
	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 PMI...

化合物

Cat.No: T11909

Synonym: FP3FBZ

Target: Opioid Receptor

Cat.No: TQ0082

Synonym: LY-2456302,CERC-501

Target: Opioid Receptor

ZT 52656A hydrochloride

Cat.No: T13414

Target: Opioid Receptor

Naloxone hydrochloride

Cat.No: T0102

Synonym: 盐酸纳洛酮,Naloxone HCl

Target: Opioid Receptor

Difelikefalin acetate

Cat.No: TP2501

Synonym: Difelikefalin acetate(1024828-77-0 free base),CR 845 acetate,Difelikefalin醋酸盐,FE 202845 acetate

Target: Opioid Receptor

Trimebutine maleate

Cat.No: T1197

Synonym: Debridat,Polibutin,马来酸曲美布汀

Target: Calcium Channel, Opioid Receptor

Cat.No: T28094

Cat.No: T34877

Synonym: KC-5103,KC5103,dl-Tifluadom,KC 5103

Cat.No: T71019

Cat.No: T69799

Cat.No: T69886

Cat.No: T69818

Eptazocine hydrobromide

Cat.No: T24035

Synonym: MCV 4169,ST-2121,MCV-4169,sT 2121, l-,l-ST-2121

Cat.No: T73339

Synonym: HSK21542

Cat.No: T27079

Synonym: FE200665,CR-665,JNJ-38488502,CR665,FE-200665,JNJ38488502

Cat.No: T25354

Synonym: Dup-747,Dup747

Cat.No: T79848

Target: Opioid Receptor

Cat.No: T71370

Leumorphin, human

Cat.No: T81938

Target: Opioid Receptor

JDTic dihydrochloride

Cat.No: T11721L

Target: JAK

Norbinaltorphimine

Cat.No: T71523

Cat.No: T69851

Cat.No: T28313

Synonym: PD-117302,PD117302

Cat.No: T73522

Synonym: FE 200665,JNJ 38488502 ; FE 200665,JNJ 38488502

Cat.No: T27027

Synonym: CJ15,208,CJ-15,208,CJ 15,208.c[Phe-D-Pro-Phe-Trp]

Cat.No: T38419

Synonym: CR-845,FE-202845

U-54494A hydrochloride

Cat.No: T36372

R-84760 hydrochloride

Cat.No: T28495

Synonym: R84760,R 84760,R 86436,R-86436,R86436

(N-Me-Tyr1,N-Me-Arg7,D-Leu-NHEt8)-Dynorphin A (1-8)

Cat.No: T76631

Dynorphin A TFA

Cat.No: T75916

Cat.No: T27934

Synonym: LY-255582,LY 255582

Target: Opioid Receptor

Endomorphin 1 acetate

Cat.No: T72423

Enadoline (Free Base)

Cat.No: T71491

Cat.No: T69798

Cat.No: T4633

Synonym: EMD-61753,阿西马朵林

Target: Opioid Receptor

CSD-CH2(1,8)-NH2

Cat.No: T80421

Target: Opioid Receptor

(+/-)-PPCC oxalate

Cat.No: T37013

Cat. No.	Product Name	Target	Signaling Pathways
T6S1010	Allomatrine 槐定碱,别苦参碱	Others	Others
	Allomatrine 是一种来源槐花树皮的生物碱。它能够激活 κ-阿片受体，进而产生缓解疼痛的作用。
T2870	Matrine Vegard,苦参碱,Matridin-15-one,Matrinium,α-Matrine,(+)-Matrine	Mitophagy; Ferroptosis; Opioid Receptor; Autophagy	Apoptosis; Autophagy; Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	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。
T3417	Amentoflavone Didemethyl-ginkgetin,穗花杉双黄酮,Amenthoflavone,3',8''-Biapigenin	Apoptosis; P450; Phospholipase; Reactive Oxygen Species; Opioid Receptor; COX; Antibacterial; RSV; Antifungal	Apoptosis; Endocrinology/Hormones; GPCR/G Protein; Immunology/Inflammation; Metabolism; Microbiology/Virology; Neuroscience; NF-κB
	Amentoflavone (3',8''-Biapigenin) 是一种具有很多生物活性的双黄酮类天然产物，有抗炎、抗氧化和神经保护等作用。
TN3367	Akuammidine	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	Akuammidine shows anti-inflammatory and anti-asthmatic properties, it has opioid analgesic activity, it shows a preference for mu-opioid binding sites with Ki values of 0.6, 2.4 and 8.6 microM at mu-, delta- and kappa-opioid binding sites, respectively.
TN3368	Akuammigine	Opioid Receptor; Adrenergic Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	Akuammigine has in vitro antimalarial activity. Akuammigine competitively antagonizes the effect of noradrenaline on postsynaptic alpha-adrenoceptors, yielding pA2 values of 4.68. Akuammidine also shows a preference for mu-opioid binding sites with Ki val

天然产物

Cat.No: T6S1010

Synonym: 槐定碱,别苦参碱

Target: Others

Cat.No: T2870

Synonym: Vegard,苦参碱,Matridin-15-one,Matrinium,α-Matrine,(+)-Matrine

Target: Mitophagy, Ferroptosis, Opioid Receptor, Autophagy

Cat.No: T3417

Synonym: Didemethyl-ginkgetin,穗花杉双黄酮,Amenthoflavone,3',8''-Biapigenin

Target: Apoptosis, P450, Phospholipase, Reactive Oxygen Species, Opioid Receptor, COX, Antibacterial, RSV, Antifungal

Cat.No: TN3367

Target: Opioid Receptor

Cat.No: TN3368

Target: Opioid Receptor, Adrenergic Receptor

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