Novel, highly antinociceptive hybrid compound in acute pain

• Autorzy: Kleczkowska P. , Kosson P. , Van der Eynde I. , Tsuda Y. , Tourwe D. , Lipkowski A.W.
• Języki publikacji: EN

Abstrakty

EN

The clinical treatment of various types of pain relies upon opioid analgesic, however most of them produce, in addition to the analgesic effect, several side effects such as development of dependence and addiction as well as sedation, dysphoria, and constipation. One of the solutions to these problems are chimeric compounds in which opioid pharmacophore is hybridized with other type of synergically active antinociceptor. Neurotensin-induced antinociception is not mediated through the opioid system. Therefore, hybridizing neurotensin with opioid element may result in a potent synergic antinociceptor. The opioid-neurotensin hybride analogue PK20, in which opioid and neurotensin pharmacophores partially overlapped, expresses high antinociceptive tail-flick effects after central as well as peripheral applications. The antinociceptive effects likely are result of synergistic/additive interaction of hybridized opioid and neurotensin pharmacophores.

• Wydawca: -
• Czasopismo: Acta Neurobiologiae Experimentalis
• Rocznik: 2011
• Tom: 71
• Numer: 1
• Opis fizyczny: p.163

Twórcy

autor

Kleczkowska P.

• Mossakowski Medical Research Centre, Polish Academy of Sciences, Warsaw, Poland

autor

Kosson P.

• Mossakowski Medical Research Centre, Polish Academy of Sciences, Warsaw, Poland

autor

Van der Eynde I.

• Department of Organic Chemistry, Vrije Universiteit Brussel, Brussels, Belgium

autor

Tsuda Y.

• Faculty of Pharmaceutical Sciences, Kobe Gakuin University, Kobe, Japan

autor

Tourwe D.

• Department of Organic Chemistry, Vrije Universiteit Brussel, Brussels, Belgium

autor

Lipkowski A.W.

• Mossakowski Medical Research Centre, Polish Academy of Sciences, Warsaw, Poland