New Imide 5-HT1A Receptor Ligands – Modification of Terminal Fragment Geometry

Abstract

Two sets of new o-methoxyphenylpiperazine (MPP; series a) and 1,2,3,4-tetrahydroisoquinoline (THIQ; series b) derivatives, containing various imide moieties derived from NAN190, were synthesized and evaluated in vitro for their ability to bind to the serotonin 5-HT 1A and 5-HT 2A receptors. All new derivatives from series a demonstrated high 5-HT 1A affinities, whereas THIQ analogues were much less active. With respect to 5-HT 2A receptors, three MPP derivatives presented moderate activity but the rest of the investigated compounds were practically inactive. The influence of changes in terminus geometry on 5-HT 1A receptor affinity was analyzed in regard to model compounds NAN190 and MM199.

G Protein-Coupled Receptors Incorporated into Rehydrated Diblock Copolymer Vesicles Retain Functionality

“…Reducing the final concentration of spiperone in pGUPs from 14 × 10 −6 to 14 × 10 −12 m and keeping the concentration of added agonist constant results in an expected increase in the protein functional rate ( Table 1 and Figure S11, Supporting Information). Furthermore, other known 5‐HT 1A R antagonists, methiothepin maleate (methiothepin), NAN‐190, and WAY 100635, that are known to inhibit agonist binding more strongly than spiperone also affect the protein functional rate . Thus, pGUPs as fabricated are sensitive to spiperone concentration and show a reduction in rate in the presence of other, more tightly binding, antagonists.…”

“…Furthermore, other known 5-HT 1A R antagonists, methiothepin maleate (methiothepin), NAN-190, and WAY 100635, that are known to inhibit agonist binding more strongly than spiperone also affect the protein functional rate. [20][21][22] Thus, pGUPs as fabricated are sensitive to spiperone concentration and show a reduction in rate in the presence of other, more tightly binding, antagonists.…”

Synthesis of New N-Phthalimide Substituted Tricyclic Imide Containing Isoxazoline and Bispiro Functional Group as Possible Anti-cancer Agents

“…Ocal and co-workers (1)(2)(3) have also conducted various investigations on tandospirone which is an antidepressant in Asia and has tricyclic imide structure (4)(5)(6). Imides are also very useful intermediates in the synthesis of various natural products (7)(8)(9)(10)(11)(12).…”

Synthesis and DSC study a new pyridinedicarboximide diones derivatives, obtained under various conditions

“…Moreover, many of the imides compounds show local anesthetic, analgetic, and antiinflammatory properties. Some of the derivatives are also inhibitors of the enzymes that are important in physiological processes e.g., AR-aldose reductase or caspase-3 (inhibitors of caspase-3 have been described as promising cardioprotectants, neuroprotectants, and antiarthritic agents) [1][2][3][4][5][6][7].…”