Indole-2-carboxamidines as novel NR2B selective NMDA receptor antagonists.
A novel series of indole-2-carboxamidine derivatives was prepared and identified as NR2B selective NMDA receptor antagonists. The influence of the substituents on the indole skeleton as well as the substitution of the benzyl moiety on the biological activity of the compounds was studied. Compound 5a was po active in the formalin test in mouse.
Borza
István
I
Gedeon Richter Ltd., Budapest, 10. PO Box 27, H-1475, Hungary. i.borza@richter.hu
Kolok
Sándor
S
Ignácz-Szendrei
Györgyi
G
Greiner
István
I
Tárkányi
Gábor
G
Galgóczy
Kornél
K
Horváth
Csilla
C
Farkas
Sándor
S
Domány
György
G
D000620:Aminoimidazole Carboxamide / Q000138:chemical synthesis / Q000494:pharmacology*; D000818:Animals; D002118:Calcium / Q000378:metabolism; D018929:Cell Culture Techniques; D002540:Cerebral Cortex / Q000166:cytology / Q000502:physiology; D007093:Imidazoles / Q000138:chemical synthesis / Q000494:pharmacology*; D007211:Indoles / Q000138:chemical synthesis / Q000494:pharmacology*; D016202:N-Methylaspartate / Q000494:pharmacology*; D051381:Rats; D016194:Receptors, N-Methyl-D-Aspartate / Q000037:antagonists & inhibitors*
D007093:Imidazoles; D007211:Indoles; C121001:NR2B NMDA receptor; D016194:Receptors, N-Methyl-D-Aspartate; D000620:Aminoimidazole Carboxamide; D016202:N-Methylaspartate; D002118:Calcium