Invention Grant
- Patent Title: N,N diethyl-N'phenylpiperazine alpha 7 and alpha 9 nicotinic acetylcholine receptor agonists and antagonists
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Application No.: US17903735Application Date: 2022-09-06
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Publication No.: US11884629B2Publication Date: 2024-01-30
- Inventor: Nicole Alana Horenstein , Roger Lee Papke , Hina Andleeb
- Applicant: University of Florida Research Foundation, Inc.
- Applicant Address: US FL Gainesville
- Assignee: University of Florida Research Foundation, Inc.
- Current Assignee: University of Florida Research Foundation, Inc.
- Current Assignee Address: US FL Gainesville
- Agency: Thomas | Horstemeyer, LLP
- Main IPC: C07D213/56
- IPC: C07D213/56 ; C07D263/32 ; C07D295/116

Abstract:
Provided are embodiments of para-substituted 1,1-dialkyl-4-phenylpiperazin-1-ium iodides advantageous for modulating inflammation that have been synthesized and their electrophysiology activities for α9, α9α10, and α7 nAChRs compared. The para position contained alkyl or aryl amides, or heterocyclic isosteres for the amide, and the alkyl groups were varied at the ammonium piperazine nitrogen to see if compensatory changes in size at this position of the molecule impacted function. The compounds were characterized with two-electrode voltage-clamp measurements on Xenopus oocytes expressing nAChRs. General, the compounds were more potent for α9-containing receptors than for α7, and the majority were either full or strong partial agonists for α9-containing nAChR.
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