Discovery and structure-activity relationships study of positive allosteric modulators of the M3 muscarinic acetylcholine receptor was written by Tanaka, Hiroaki;Negoro, Kenji;Koike, Takanori;Tsukamoto, Issei;Yokoyama, Kazuhiro;Maeda, Jun;Inagaki, Yusuke;Shimoshige, Yukinori;Ino, Katsutoshi;Ishizu, Kenichiro;Takahashi, Taisuke. And the article was included in Bioorganic & Medicinal Chemistry in 2020.Related Products of 1722-95-8 This article mentions the following:
The M3 muscarinic acetylcholine receptor (mAChR) is a member of the family of mAChRs, which are associated with a variety of physiol. functions including the contraction of various smooth muscle tissues, stimulation of glandular secretion, and regulation of a range of cholinergic processes in the central nerve system. We report here the discovery and a comprehensive structure-activity relationships (SARs) study of novel pos. allosteric modulators (PAMs) of the M3 mAChR through a high throughput screening (HTS) campaign. Compound 9(I) exhibited potent in vitro PAM activity towards the M3 mAChR and significant enhancement of muscle contraction in a concentration-dependent manner when applied to isolated smooth muscle strips of rat bladder. Compound 9 also showed excellent subtype selectivity over other subtypes of mAChRs including M1, M2, and M4 mAChRs, and moderate selectivity over the M5 mAChR, indicating that compound 9 is an M3-preferring M3/M5 dual PAM. Moreover, compound 9 displayed acceptable pharmacokinetics profiles after oral dosing to rats. These results suggest that compound 9 may be a promising chem. probe for the M3 mAChR for further investigation of its pharmacol. function both in vitro and in vivo. In the experiment, the researchers used many compounds, for example, (R)-2-Methylpiperidine (cas: 1722-95-8Related Products of 1722-95-8).
(R)-2-Methylpiperidine (cas: 1722-95-8) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. Piperidine prefers a chair conformation, similar to cyclohexane. Unlike cyclohexane, piperidine has two distinguishable chair conformations: one with the N鈥揌 bond in an axial position, and the other in an equatorial position.Related Products of 1722-95-8
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem