Synthesis of 5-HT3 receptor antagonists, [11C]Y-25130 and [11C]YM060
β Scribed by Kiichi Ishiwata; Kenji Ishii; Shin-Ichi Ishii; Michio Senda
- Publisher
- Elsevier Science
- Year
- 1995
- Tongue
- English
- Weight
- 271 KB
- Volume
- 46
- Category
- Article
- ISSN
- 0969-8043
No coin nor oath required. For personal study only.
π SIMILAR VOLUMES
MDL 72222, an antagonist of 5HT3 receptors, was labeled with a specific radioactivity of 340-400 mCi/mumol by alkylation of the nor-precursor with [11C]CH3I. The yield of the synthesis, starting from [11C]methyliodide to the purified product and corrected for decay, was good approximately 70-75%. Af
DR4446 (1-methyl-2a-[4-(4,5,6,7-tetrahydrothieno[3,2-c]pyridin-5-yl)butyl]-2a, 3,4,5-tetrahydro-1H-benz[cd ]indole-2-one) is a potent 5-HT 7 receptor antagonist (K i ΒΌ 9:7 nM) with a high selectivity over other 5-HT family receptors (K i for 5-HT 1A : 770 nM; for other 5-HT receptors: >1000 nM). As
## Abstract Syntheses of labelled versions of 5βHT~3~ receptor antagonists, Alosetron and Lurosetron, are described. [^14^C]Alosetron was prepared by routes utilizing either Fischer indolisation of an amidohydrazine or palladiumβmediated cyclisation of an aryl enaminone as key steps. ^2^H and ^13^C