Bioorganic and Medicinal Chemistry Letters p. 2595 - 2600 (1996)
Update date:2022-08-03
Topics:
Mazurov, Anatoly A.
Andronati, Sergei A.
Korotenko, Tamara I.
Sokolenko, Nikolai I.
Dyadenko, Alexei I.
Shapiro, Yuri E.
Gorbatyuk, Vitalii Ya.
Voronina, Tatyana A.
A new cognitive enhancer (8S, 10aS)-8-carbamoyl-1,2,3,6,7,8,9,10a-octahydro-5H,10H-pyrrolo[1,2-a][1, 4]diazocin-5,10-dione (3) has been designed based on the approach consisting of two steps: 1) 'obligatory' replacement of histidine with glutamine in TRH; 2) the application of conformational constraints for putative bioactive conformation of [Gln2]-TRH. 3 reversed on 100% electroconvulsive shock-induced amnesia at doses of 0.1 and 1.0 mg/kg and on 83% scopolamine-induced amnesia at a dose of 1 mg/kg, using passive avoidance test.
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Doi:10.1007/BF02256763
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(1997)
