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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).
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.
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
关键词: GNTI dihydrochloride, GNTI dihydrochloride supplier, Potent, selective, κ-opioid, kappa-opioid, antagonists, KOP, Receptors, OP2, Kappa, Opioid, 1282, Tocris Bioscience
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
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Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.
The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.