[Indoles. 10. Synthesis, structure and D2-affinity of beta-carboline analogs of flutroline].
10 is a beta-carboline analogue of the neuroleptic flutroline2a,b) with significant lower affinity at the dopamine D2 binding site. Various synthetic routes to 10 and the solid state structure of 8 are described, structure activity relations, in particular the importance of the "S-shape" and the rigid dopamine conformation are discussed.
Lehmann
J
J
Pharmazeutisches Institut, Universität Bonn.
Knoch
F
F
Jiang
N
N
D014150:Antipsychotic Agents / Q000737:chemistry* / Q000494:pharmacology; D002243:Carbolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D065127:Dopamine D2 Receptor Antagonists; D008968:Molecular Conformation; D017448:Receptors, Dopamine D2 / Q000737:chemistry; D013329:Structure-Activity Relationship
D014150:Antipsychotic Agents; D002243:Carbolines; D065127:Dopamine D2 Receptor Antagonists; D017448:Receptors, Dopamine D2; C026240:flutroline
Indole, 10. Mitt. Synthese, Struktur und D2-Affinität des beta-Carbolin-Analogons von Flutrolin.