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| N-2′-Indolylnaltrexamine ： ウィキペディア英語版 |
N-2′-Indolylnaltrexamine
''N''-2′-Indolylnaltrexamine (INTA) is an opioid and derivative of β-naltrexamine. This molecule is loosely derived from the classical opioid morphine. This experimental drug candidate is under developed as a κ-opioid receptor agonist for pain management with fewer adverse side effects. Preclinical study in mice showed potent analgesic effects with no tolerance or dependence. The mice also showed no adverse effects in the conditioned place aversion assay.
==Action==
INTA acts on the body by binding to a G-protein coupled receptor (GPCR) called the opioid receptor.〔Le, Naour M, MM Lunzer, MD Powers, AE Kalyuzhny, MA Benneyworth, MJ Thomas, and PS Portoghese. "Putative Kappa Opioid Heteromers As Targets for Developing Analgesics Free of Adverse Effects." Journal of Medicinal Chemistry. 57.15 (2014): 6383-92〕 Opioid Receptors, themselves, are divided into different subunits: kappa (KOR), delta (DOR), and mu (MOR) receptors.〔Carvey, Paul M. Drug Action in the Central Nervous System. Oxford: Oxford University Press, 1998.〕 When INTA binds to the receptors, it is actually binding to a heteromer of the receptor. This means that it is binding to two of the subunits, instead of just one. These two receptors "work together" to form a conformation to block the recruitment of a protein family known as the β-arrestins.〔 These proteins are responsible for the regulation of GPCR's and they cause the internalization of the receptor to prevent further activation, leading to an increased tolerance to opioid drugs.〔van Koppen, C. J.; Jakobs, K. H. Arrestin-Independent Internalization of G Protein-Coupled Receptors. Molecular Pharmacology 2004, 66, 365-367〕
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