AT-076
In this article we are going to explore AT-076 in depth, a topic that has generated great interest and debate in recent times. From its origins to its relevance today, AT-076 has been the subject of study and analysis in different areas. Through this article, we seek to shed light on this topic, addressing different perspectives and approaches that allow us to better understand its importance and impact in different contexts. To do this, we will rely on the vision of experts, studies and relevant data that will help us delve into the ins and outs of AT-076 and reflect on its relevance in contemporary society.
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| Formula | C26H35N3O3 |
| Molar mass | 437.584 g·mol−1 |
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AT-076 is a so-called opioid "pan" antagonist and is the first reasonably balanced antagonist known of all four opioid receptor types.[1] It acts as a silent antagonist of all four of the opioid receptors, behaving as a competitive antagonist of the μ-opioid receptor (Ki = 1.67 nM) and δ-opioid receptor (Ki = 19.6 nM) and as a noncompetitive antagonist of the κ-opioid receptor (Ki = 1.14 nM) and nociceptin receptor (Ki = 1.75 nM).[1] AT-076 was derived from the selective κ-opioid receptor antagonist JDTic via removal of the 3,4-dimethyl group of the trans-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine antagonist scaffold which increased affinity for the nociceptin receptor by 10-fold and for the μ- and δ-opioid receptors by 3-6-fold.[1]
See also
References
- ^ a b c Zaveri NT, Journigan VB, Polgar WE (2015). "Discovery of the First Small-Molecule Opioid Pan Antagonist with Nanomolar Affinity at Mu, Delta, Kappa, and Nociceptin Opioid Receptors". ACS Chem Neurosci. 6 (4): 646–57. doi:10.1021/cn500367b. PMC 4401318. PMID 25635572.
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