Author/Authors :
Guy Van Lommen، نويسنده , , Marcel De Bruyn، نويسنده , , Marc Schroven، نويسنده , , Wim Verschueren، نويسنده , , Walter Janssens، نويسنده , , Jan Verrelst، نويسنده , , Josée Leysen، نويسنده ,
Abstract :
The synthesis and SAR of a series of non-indole 5HT1D agonists is described. The most interesting molecule of this series is compound 13, alniditan. It is active as a constrictor of the saphenous vein of the dog and of the pig basilar artery with ED50 values of 9.09×10−9M and 2.29×10−8M respectively, and it has high affinities to the 5HT1D-receptor and to the 5HT1D-receptor with pKi values of 8.6 and 8.3 respectively.
