TY - JOUR AU - Lengyel, Miklós AU - Erdélyi, Ferenc AU - Pergel, Enikő AU - Polonkáné Bálint, Ágnes AU - Dobolyi, Alice AU - Bozsaki, Peter AU - Dux, Mária AU - Király, Kornél P AU - Hegedűs, Tamás AU - Czirják, Gábor AU - Mátyus, Péter AU - Enyedi, Péter TI - Chemically Modified Derivatives of the Activator Compound Cloxyquin Exert Inhibitory Effect on TRESK (K2P18.1) Background Potassium Channel JF - MOLECULAR PHARMACOLOGY J2 - MOL PHARMACOL VL - 95 PY - 2019 IS - 6 SP - 652 EP - 660 PG - 9 SN - 0026-895X DO - 10.1124/mol.118.115626 UR - https://m2.mtmt.hu/api/publication/30654928 ID - 30654928 AB - Cloxyquin has been reported as a specific activator of TRESK (K2P18.1, TWIK-related spinal cord K+ channel) background potassium channel. In this study, we have synthetized chemically modified analogues of cloxyquin and tested their effects on TRESK and other K2P channels. The currents of murine K2P channels, expressed heterologously in Xenopus oocytes, were measured by two-electrode voltage clamp, whereas the native background K+ conductance of mouse dorsal root ganglion (DRG) neurons was examined by the whole-cell patch clamp method. Some of the analogues retained the activator character of the parent compound, but more interestingly, other derivatives inhibited mouse TRESK current. The inhibitor analogues (A2764 and A2793) exerted state-dependent effect. The degree of inhibition by 100 µM A2764 (77.8±1.5%, n=6) was larger in the activated state of TRESK (i.e. after calcineurin-dependent stimulation) than in the resting state of the channel (42.8±4.3% inhibition, n=7). The selectivity of the inhibitor compounds was tested on several K2P channels. A2793 inhibited TASK-1 (100 µM, 53.4±6%, n=5), while A2764 was more selective for TRESK, it only moderately influenced TREK-1 and TALK-1. The effect of A2764 was also examined on the background K+ currents of DRG neurons. A subpopulation of DRG neurons, prepared from wild-type animals, expressed background K+ currents sensitive to A2764, while the inhibitor did not affect the currents in the DRG neurons of TRESK-deficient mice. Accordingly, A2764 may prove to be useful for the identification of TRESK current in native cells, and for the investigation of the role of the channel in nociception and migraine. LA - English DB - MTMT ER - TY - JOUR AU - Mátyus, Péter AU - Polonkáné Bálint, Ágnes AU - Dunkel, Petra AU - Földi, Á AU - Ludányi, K AU - Bényei, Cs A TI - Aza-ring annelation via type 2 tert-amino effect: mechanism and scope JF - BOLETÍN DE LA SOCIEDAD QUÍMICA DE MÉXICO J2 - B SOC QUIM MEX VL - 5 PY - 2011 IS - 3 SP - 37 EP - 37 PG - 1 SN - 1870-1809 UR - https://m2.mtmt.hu/api/publication/2855891 ID - 2855891 LA - English DB - MTMT ER - TY - GEN AU - Mátyus, Péter AU - Dunkel, Petra AU - Polonkáné Bálint, Ágnes AU - Földi, Á AU - Deme, Ruth AU - Gyires, Klára AU - Magyar, K AU - Tábi, T AU - Szökő, É TI - Semicarbazide-sensitive amine oxidase/vascular adhesion protein-1 inhibitors as novel anti-inflammatory agents PY - 2011 UR - https://m2.mtmt.hu/api/publication/1753121 ID - 1753121 LA - English DB - MTMT ER - TY - GEN AU - Földi, ÁA AU - Polonkáné Bálint, Ágnes AU - Drahos, László AU - Mátyus, Péter TI - Váratlan termékek képződése vinilcsoporttal szubsztituált tercier arilaminokból PY - 2010 UR - https://m2.mtmt.hu/api/publication/2029634 ID - 2029634 LA - Hungarian DB - MTMT ER - TY - GEN AU - Deme, Ruth AU - Polonkáné Bálint, Ágnes AU - Földi, ÁA AU - Dunkel, Petra AU - Mátyus, Péter TI - terc-amino effektus alkalmazása policiklusos vegyületek előállítására PY - 2010 UR - https://m2.mtmt.hu/api/publication/2027325 ID - 2027325 LA - Hungarian DB - MTMT ER - TY - GEN AU - Deme, Ruth AU - Dunkel, Petra AU - Polonkáné Bálint, Ágnes AU - Mátyus, Péter TI - Azocin és azecin gyűrűrendszerek előállítása a terc-amino effektus alkalmazásával PY - 2009 UR - https://m2.mtmt.hu/api/publication/2027279 ID - 2027279 N1 - [Poszter] LA - Hungarian DB - MTMT ER - TY - JOUR AU - Franck, P AU - Hostyn, S AU - Dajka-Halasz, B AU - Polonkáné Bálint, Ágnes AU - Monsieurs, K AU - Mátyus, Péter AU - Maes, BUW TI - Pd-catalyzed intramolecular direct arylations at high temperature JF - TETRAHEDRON J2 - TETRAHEDRON VL - 64 PY - 2008 IS - 26 SP - 6030 EP - 6037 PG - 8 SN - 0040-4020 DO - 10.1016/j.tet.2008.01.060 UR - https://m2.mtmt.hu/api/publication/1344109 ID - 1344109 LA - English DB - MTMT ER - TY - JOUR AU - Polonkáné Bálint, Ágnes AU - Saraceno, C AU - Ludányi, Krisztina AU - Bényei, Attila Csaba AU - Mátyus, Péter TI - Novel Extensions of the tert-Amino Effect: Formation of Phenanthridines and Diarene-Fused Azocines from ortho-ortho′-Functionalized Biaryls JF - SYNLETT J2 - SYNLETT VL - 2008 PY - 2008 IS - 18 SP - 2846 EP - 2850 PG - 5 SN - 0936-5214 DO - 10.1055/s-0028-1083537 UR - https://m2.mtmt.hu/api/publication/1189926 ID - 1189926 N1 - Megjegyzés-22050677 Z9: 13 AB - Phenanthridines and azocines fused to two benzene rings or one benzene and one pyridazinone ring, which are otherwise difficult to access, were prepared via two new extensions of the tert-amino effect. The synthetic pathway includes three steps: i) Suzuki reaction of an ortho-functionalized phenylboronic acid with ortho-disubstituted benzenes or pyridazinones; ii) the Knoevenagel condensation reaction of the biaryl aldehydes formed with active methylene compounds to obtain vinyl derivatives or, through their cyclization, phenanthridines via a tert-amino effect; and iii) thermal isomerization of vinyl or phenanthridinium compounds to fused azocines via another type of tert-amino effect. LA - English DB - MTMT ER - TY - GEN AU - Polonkáné Bálint, Ágnes AU - Dunkel, Petra AU - Mátyus, P TI - Új típusú azocin és azecin gyűrűrendszerek előállítása új úton: a terc-amino effektus kiterjesztése PY - 2007 UR - https://m2.mtmt.hu/api/publication/1344145 ID - 1344145 N1 - [Előadás] LA - Hungarian DB - MTMT ER - TY - GEN AU - Polonkáné Bálint, Ágnes AU - Saraceno, C AU - Czugler, Mátyás AU - Mátyus, Péter TI - Syntheses of dibenzazocines and a pyridazino-fused benzazocine by application of a new type of tert-amino effect PY - 2006 UR - https://m2.mtmt.hu/api/publication/1344144 ID - 1344144 N1 - [Előadás] LA - English DB - MTMT ER -