C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 451/02 (2006.01) A61K 31/46 (2006.01) A61K 31/555 (2006.01) A61K 51/00 (2006.01) A61K 51/04 (2006.01) C07F 7/22 (2006.01)
Patent
CA 2254089
The invention features tropane derivatives useable in particular for in vivo detection of dopamine transporters. These derivatives are of formula (I), in which R?1¿ is I or Sn(R?3¿)¿3?, R?2¿ is for instance the methyl group, and X and Y are various substituents. The derivatives with X = CH¿3? and Y = H present a high specificity for the dopamine transporter relative to that of serotonin (74 % inhibition when the transporter is previously saturated with GBR 12909)
L'invention concerne des dérivés du tropane utilisables en particulier pour la détection in vivo des transporteurs de la dopamine. Ces dérivés répondent à la formule (I), dans laquelle R1 est I ou Sn(R3)3, R2 est par exemple le groupe méthyle, et X et Y sont divers substituants. Les dérivés avec X = CH3 et Y = H présentent une forte spécificité pour le transporteur de la dopamine par rapport à celui de la sérotonine (inhibition de 74 % lorsque le transporteur est saturé préalablement par GBR 12909).
Besnard Jean-Claude
Emond Patrick
Frangin Yves
Guilloteau Denis
Mauclaire Laurent
Cis Bio International
Goudreau Gage Dubuc
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