GNTI dihydrochloride

Discontinued Product

1282 has been discontinued.

说明: Potent, selective κ antagonist
化学名: 5'-Guanidinyl-17-(cyclopropylmethyl)-6,7-dehydro-4,5α-epoxy-3,14-dihydroxy-6,7-2',3'-indolomorphinan dihydrochloride
纯度: ≥96% (HPLC)
说明书
引用文献 (1)
评论 (1)
文献 (2)

生物活性 for GNTI dihydrochloride

GNTI dihydrochloride is a highly potent κ opioid receptor antagonist (Ki = 0.18 nM for human cloned κ receptors expressed in CHO cells). Displays 208- and 799-fold selectivity over μ and δ receptors respectively. Reduces feeding behavior in rats with a much higher potency (300-30,000-fold) and a shorter duration of action than nor-binaltorphimine (Cat.No. 0347).

技术数据 for GNTI dihydrochloride

分子量 544.48
公式 C27H29N5O3.2HCl
储存 Desiccate at -20°C
纯度 ≥96% (HPLC)
CAS Number 351183-88-5
PubChem ID 90479777
InChI Key GJPIMNXJPMPQHK-CVVXFVLRSA-N
Smiles OC3=CC=C2CC([C@@]5(O)[C@@]4(CC8)C2=C3O[C@H]4C(NC7=C6C=C(NC=N)C=C7)=C6C5)N8CC1CC1.Cl.Cl

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

产品说明书 for GNTI dihydrochloride

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参考文献 for GNTI dihydrochloride

参考文献是支持产品生物活性的出版物。

Jewett et al (2001) The kappa-opioid antagonist GNTI reduces U50,488-, DAMGO-, and deprivation-induced feeding, but not butorphanol- and neuropeptide Y-induced feeding in rats. Brain Res. 909 75 PMID: 11478923

Jones et al (1998) Mutational evidence for a common κ antagonist binding pocket in the wild type κ and mutant μ[K303E] opioid receptors. J.Med.Chem. 41 4911 PMID: 9836606

Jones and Portoghese (2000) 5'-Guanidinonaltrindole, a highly selective and potent κ-opioid receptor antagonist. Eur.J.Pharmacol. 396 49 PMID: 10822054

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关键词: GNTI dihydrochloride, GNTI dihydrochloride supplier, Potent, selective, κ-opioid, kappa-opioid, antagonists, KOP, Receptors, OP2, Kappa, Opioid, 1282, Tocris Bioscience

1 篇 GNTI dihydrochloride 的引用文献

引用文献是使用了 Tocris 产品的出版物。 GNTI dihydrochloride 的部分引用包括:

Choi et al (2010) Roles of opioid receptor subtype in the spinal antinociception of selective cyclooxygenase 2 inhibitor. Korean J Pain 23 236 PMID: 21217886


GNTI dihydrochloride 的评论

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Very Good Product.
By Luca Zangrandi on 01/14/2020
分析类型: Ex Vivo
种属: Human

Successfully stopped selective agonist-induced ERK phosphorylation in CHO cells.

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