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Tytuł oryginału: Novel N-{omega-[4-(2-methoxyphenyl)piperazin-1-yl]-ethyl}pyrid-2(1H)-ones with diversified 5-HT 1A receptor activity.
Autorzy: Paluchowska Maria H., Bugno Ryszard, Charakchieva-Minol Sijka, Wesołowska Anna, Chojnacka-Wójcik Ewa
Źródło: Pol. J. Pharmacol. 2002: 54 (6) s.641-646, il., tab., bibliogr. 22 poz.
Sygnatura GBL: 313,156

Hasła klasyfikacyjne GBL:
  • farmacja

    Typ dokumentu:
  • praca doświadczalna
  • tytuł obcojęzyczny

    Wskaźnik treści:
  • zwierzęta
  • szczury
  • płeć męska
  • in vitro

    Streszczenie angielskie: Novel omega-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl derivatives 1-6 containing 4-, 5- and/or 6-arylsubstituted pyrid-2(1H)-one moiety were synthesized. All the new compounds were examined in vitro to assess their 5-HT 1A and 5-HT 2A receptor affinities. Compounds 3 and 4 with a 5- or a 6-phenylsubstituted pyridone ring demonstrated high 5-HT 1A receptor affinity (Ki=17 and 38 nM, respectively) and were tested in behavioral functional models. Derivative 3 can be regarded as a weak 5-HT 1A postsynaptic antagoninist, whereas 4 showed features of a weak partial agonist of 5-HT 1A receptors (an agonist of pre- and an antagonist of posstynaptic ones). Binding affinities and in vivo results were discussed in comparison with those for the previously described tetramethylene analogs. The obtained results showed that the shortening of the aliphatic chain to two methylene groups exposed the intrinsic activity of the ligand 4 and 5-HT 1A receptor sites.

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