On December 4, 2003, Orjales, Aurelio; Mosquera, Ramon; Toledo, Antonio; Pumar, M. Carmen; Garcia, Neftali; Cortizo, Lourdes; Labeaga, Luis; Innerarity, Ana published an article.Category: chlorides-buliding-blocks The title of the article was Syntheses and Binding Studies of New [(Aryl)(aryloxy)methyl]piperidine Derivatives and Related Compounds as Potential Antidepressant Drugs with High Affinity for Serotonin (5-HT) and Norepinephrine (NE) Transporters. And the article contained the following:
In a wide search program toward new, efficient, and fast-acting antidepressant drugs, series of new compounds having an (aryl)(aryloxy)methyl moiety linked directly or through a methylene chain to different substituted and unsubstituted cycles (isoquinoline, piperazine, piperidine, tetrahydropyran, or cyclopentane) were prepared These compounds have been evaluated for their affinities for serotonin (5-HT) transporter (SERT) and 5-HT1A and 5-HT2A receptors. Racemic mixtures of 4-[(aryl)(aryloxy)methyl]piperidines I (R1 = H, Me, MeCO; R2 = H, 3-F, 4-F, 4-Cl, 4-Me; R3 = H, 2-CN, 4-O2N, 4-MeO, 2-Ph, etc.) showed much higher affinity values for SERT than fluoxetine and resulted in lack of affinity for 5-HT1A and 5-HT2A receptors. Some of these racemic mixtures were resolved to their enantiomers and tested for binding to norepinephrine (NE) transporter (NET), dopamine (DA) transporter (DAT), and α2 receptor. Several of these enantiomers, (-)-I (R1 = R2 = H; R3 = 2-F), (-)-I (R1 = R2 = H; R3 = 3-F), (-)-I (R1 = H; R2 = 3-F; R3 = 2-F), (+)-I (R1 = H; R2 = R3 = 3-F), displayed a dual binding profile with affinities for SERT and NET with Ki < 25 nM and a NET/SERT ratio <10. (-)-I (R1 = R2 = H; R3 = 3-F) (coded as F-98214-TA for development studies) showed a dual binding profile with very high affinity values for SERT and NET (Ki = 1.9 and 13.5 nM, resp.), and further pharmacol. characterization is in progress for its evaluation as a antidepressant. The experimental process involved the reaction of 4-Chloro-2-fluorotoluene(cas: 452-75-5).Category: chlorides-buliding-blocks
The Article related to piperidine aryloxyalkyl preparation antidepressant serotonin norepinephrine transporter affinity, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Category: chlorides-buliding-blocks
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