《Discovery and Structure-Activity Relationships of Nociceptin Receptor Partial Agonists That Afford Symptom Ablation in Parkinson’s Disease Models》 was written by Kamakolanu, Uma Gayathri; Meyer, Michael E.; Yasuda, Dennis; Polgar, Willma E.; Marti, Matteo; Mercatelli, Daniela; Pisano, Clarissa Anna; Brugnoli, Alberto; Morari, Michele; Zaveri, Nurulain T.. Electric Literature of C3H8ClNO And the article was included in Journal of Medicinal Chemistry in 2020. The article conveys some information:
A novel series of C(3)-substituted piperdinylindoles were developed as nociceptin opioid receptor (NOP) partial agonists to explore a pharmacol. hypothesis that NOP partial agonists would afford a dual pharmacol. action of attenuating Parkinson’s disease (PD) motor symptoms and development of levodopa-induced dyskinesias. SAR around the C-3 substituents investigated effects on NOP binding, intrinsic activity, and selectivity and showed that while the C(3)-substituted indoles are selective, high affinity NOP ligands, the steric, polar, and cationic nature of the C-3 substituents affected intrinsic activity to afford partial agonists with a range of efficacies. Compounds 4, 5, and 9 with agonist efficacies between 25% and 35% significantly attenuated motor deficits in the 6-OHDA-hemilesioned rat model of PD. Further, unlike NOP antagonists, which appear to worsen dyskinesia expression, these NOP partial agonists did not attenuate or worsen dyskinesia expression. The NOP partial agonists and their SAR reported here may be useful to develop nondopaminergic treatments for PD. In addition to this study using Azetidin-3-ol hydrochloride, there are many other studies that have used Azetidin-3-ol hydrochloride(cas: 18621-18-6Electric Literature of C3H8ClNO) was used in this study.
Azetidin-3-ol hydrochloride(cas:18621-18-6) is one of azetidine.Azetidines (azacyclobutanes) constitute a well-known class of heterocyclic compounds. Azetidine scaffold has been discovered in several natural products.Electric Literature of C3H8ClNO Several pharmacologically important synthetic compounds also contain azetidine ring. Because of inherent ring strain, the synthesis of azetidines is a challenging endeavor.
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