Chemistry:AT-076
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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 an antagonist of all four types of opioid receptor, 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 (NOP, Ki = 1.75 nM).[1] AT-076 was derived from the κ-opioid receptor antagonist JDTic, which showed affinity for NOP,[2] by removal of two methyl groups from the piperidine ring. This increased affinity for NOP 10-fold relative to the parent compound.[1]
See also
References
- ↑ 1.0 1.1 1.2 "Discovery of the First Small-Molecule Opioid Pan Antagonist with Nanomolar Affinity at Mu, Delta, Kappa, and Nociceptin Opioid Receptors". ACS Chemical Neuroscience 6 (4): 646–657. 2015. doi:10.1021/cn500367b. PMID 25635572.
- ↑ "Selective κ opioid antagonists nor-BNI, GNTI and JDTic have low affinities for non-opioid receptors and transporters". PLOS ONE 8 (8). 2013. doi:10.1371/journal.pone.0070701. PMID 23976952.
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