SAR exploration of the non-imidazole histamine H3 receptor ligand ZEL-H16 reveals potent inverse agonism was written by Wagner, Gabor;Mocking, Tamara A. M.;Ma, Xiaoyuan;Slynko, Inna;Da Costa Pereira, Daniel;Breeuwer, Robin;Rood, Niek J. N.;van der Horst, Cas;Vischer, Henry F.;de Graaf, Chris;de Esch, Iwan J. P.;Wijtmans, Maikel;Leurs, Rob. And the article was included in Archiv der Pharmazie (Weinheim, Germany).Name: 1-(3-Chloropropyl)piperidine hydrochloride This article mentions the following:
Histamine H3 receptor (H3R) agonists without an imidazole moiety remain very scarce. Of these, ZEL-H16 (1) has been reported previously as a high-affinity non-imidazole H3R (partial) agonist. Our structure-activity relationship anal. using derivatives of 1 identified both basic moieties as key interaction motifs and the distance of these from the central core as a determinant for H3R affinity. However, in spite of the reported H3R (partial) agonism, in our hands, 1 acts as an inverse agonist for G伪i signaling in a CRE-luciferase reporter gene assay and using an H3R conformational sensor. Inverse agonism was also observed for all of the synthesized derivatives of 1. Docking studies and mol. dynamics simulations suggest ionic interactions/hydrogen bonds to H3R residues D1143.32 and E2065.46 as essential interaction points. In the experiment, the researchers used many compounds, for example, 1-(3-Chloropropyl)piperidine hydrochloride (cas: 5472-49-1Name: 1-(3-Chloropropyl)piperidine hydrochloride).
1-(3-Chloropropyl)piperidine hydrochloride (cas: 5472-49-1) belongs to piperidine derivatives. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Name: 1-(3-Chloropropyl)piperidine hydrochloride
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem