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GPCR / G Protein /
Opioid Receptors

Opioid Receptors

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AR-M 1000390 hydrochloride

Catalog No. A21911
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δ opioid receptor agonist

AR-M 1000390 hydrochloride is an exceptionally selective, potent δ opioid receptor agonist with an EC50 of 7.2??0.9 nM for δ agonist potency. 了解更多

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CYT-1010 hydrochloride

Catalog No. A21348
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mu-opioid receptor agonist

CYT-1010 hydrochloride is a mu-opioid receptor agonist extracted from patent WO2013173730A2, with EC50s of 13.1 nM and 0.0053 nM on beta-arrestin recruitment and inhibition of cAMP production, respectively. 了解更多

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DPI-3290

Catalog No. A13699
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opioid receptors agonist

DPI-3290 (Org 41793) is a potent and specific opioid receptors agonist with Ki values of 0.18 nM, 0.46 nM, and 0.62 nM for δ-, μ-, and κ-opioid receptors, respectively. 了解更多

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TRV130 HCl (Oliceridine)

Catalog No. A15444
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u-opioid receptor 激动剂

TRV130 HCl (Oliceridine)是一种新型的μ-opioid 受体（MOR）G蛋白偏向配体。诱导强大的G蛋白信号传导（pEC50 = 8.1），效力和功效与吗啡相似，但β-arrestin募集和受体内在化作用要低得多。了解更多

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- Preeti Manandhar, .et al. Tapentadol shows lower intrinsic efficacy at μ receptor than morphine and oxycodone, Pharmacol Res Perspect, 2022, 10:e00921 PMID: 35084120
- Li He, .et al. Pharmacological and genetic manipulations at the ?-opioid receptor reveal arrestin-3 engagement limits analgesic tolerance and does not exacerbate respiratory depression in mice, Neuropsychopharmacology, 2021, 13 July PMID: 34257415
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Trimebutine maleate

Catalog No. A18115
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?- opioid receptor agonist

Trimebutine Maleate is a drug with antimuscarinic and weak mu opioid agonist effects. Trimebutine Maleate modulates the calcium and potassium channels, relieves abdominal pain in patients with irritable bowel syndrome. 了解更多

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Cebranopadol (GRT-6005)

Catalog No. A12670
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Opioid Receptor 激动剂

Cebranopadol是一种有效的伤害感受器/孤儿蛋白FQ肽（NOP）和阿片受体激动剂。作用于人NOP，MOP，KOP 和δ-阿片肽(DOP)受体，Ki/EC50 分别为 0.9 nM/13 nM，0.7 nM/1.2 nM，2.6 nM/17 nM，18 nM/110 nM。了解更多

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Alvimopan monohydrate

Catalog No. A14992
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?-opioid receptor 激动剂

Alvimopan monohydrate是一种外围作用的类阿片受体（PAM-OR，IC50 = 1.7 nM）拮抗剂，可促进术后肠胃的恢复。了解更多

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Alvimopan dihydrate

Catalog No. A14991
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?-opioid receptor 激动剂

Alvimopan dihydrate (LY 246736,ADL 8-2698)是一种外周作用的类阿片受体（PAM-OR，IC50 = 1.7 nM）拮抗剂，可促进术后胃肠道恢复。了解更多

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ADL5747

Catalog No. A13479
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δ opioid receptor 激动剂

ADL5747是一种选择性的非肽类δ opioid激动剂。了解更多

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U-69593

Catalog No. A14187
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κ1-opioid receptor 激动剂

U-69593是有效的选择性κ1阿片受体激动剂（EC50 = 80-109 nM）。在体内有活性。抗伤害感受。了解更多

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Nalmefene hydrochloride

Catalog No. A13843
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dopamine receptor 激动剂

Nalmefene hydrochloride是opioid receptor拮抗剂。了解更多

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- Mark G Papich, .et al. Naloxone and nalmefene absorption delivered by hollow microneedles compared to intramuscular injection, Drug Deliv Transl Res, 2022, Feb;12(2):376-383 PMID: 34817831
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Nalfurafine hydrochloride

Catalog No. A12579
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opioid κ-selective 激动剂

Nalfurafine hydrochloride是一种κ-opioid激动剂。了解更多

Product Citations (6)

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- Alexander R French, .et al. Sex- and β-arrestin-dependent effects of kappa opioid receptor-mediated ethanol consumption, Pharmacol Biochem Behav, 2022, May;216:173377 PMID: 35364122
- Wen-Wen Zhang, .et al. Peripheral ablation of type III adenylyl cyclase induces hyperalgesia and eliminates KOR-mediated analgesia in mice, JCI Insight, 2022, Feb 8;7(3):e153191 PMID: 34914639
- A Dunn, .et al. Modulation of Cocaine-Related Behaviors by Low Doses of the Potent KOR Agonist Nalfurafine in Male C57BL6 Mice, Psychopharmacology (Berl), 2020, May 20 PMID: 32435819
- Dunn AD, .et al. Signaling Properties of Structurally Diverse Kappa Opioid Receptor Ligands: Toward in Vitro Models of in Vivo Responses, ACS Chem Neurosci, 2019, Aug 21;10(8):3590-3600 PMID: 31313902
- Anika Mann, .et al. Agonist-selective NOP receptor phosphorylation correlates in vitro and in vivo and reveals differential post-activation signaling by chemically diverse agonists, Sci Signal, 2019, Mar 26;12(574). pii: eaau8072 PMID: 30914485
- Snyder LM, .et al. Kappa Opioid Receptor Distribution and Function in Primary Afferents, Neuron, 2018, Sep 19;99(6):1274-1288.e6 PMID: 30236284
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BRL 52537 HCl

Catalog No. A11210
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Opioid Receptors 激动剂

BRL 52537 hydrochloride是一种高度选择性和有效的κ阿片类激动剂（Ki = 0.24 nM）。比吗啡强25倍。了解更多

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MCOPPB 3HCl

Catalog No. A10561
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NOP receptor 激动剂

MCOPPB 3HCl是一种用作伤害感受器受体的有效和选择性激动剂的化合物，pKi为10.07。了解更多

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ADL5859 HCl

Catalog No. A11072
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Opioid Receptor 激动剂

ADL5859 HCl是高效的选择性δ阿片受体激动剂，Ki值为0.84 nM，ED50值为20 nM。了解更多

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