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Fluoro analogs of WAY-100635 with varying pharmacokinetics properties.

Abstract：

:Radiolabeled derivatives of WAY-100635 have been shown to be important for imaging in vivo because of their antagonist properties and their specificity for the 5-hydroxytryptamine(1A) (5-HT(1A)) receptor. Our goal is to prepare a series of radiofluorinated derivatives of WAY-100635 that, in the rat, range in pharmacokinetic properties from nearly irreversible to reversible in their behavior. It appears that derivatives containing a cyclohexanecarboxylic acid (e.g., FCWAY) with its high affinity and high target to nontarget contrast, has properties suited to measure receptor concentration. Derivatives based on phenylcarboxamide (e.g., FBWAY and MeFBAWAY) have properties more suited to the measurement of changes in endogenous serotonin. The compound containing the pyrimidine moiety in place of the pyridine moeity in FBWAY (FBWAY 1,3N) appears to have intermediate properties.

journal_name

Nucl Med Biol

journal_title

Nuclear medicine and biology

authors

Lang L,Jagoda E,Schmall B,Sassaman M,Ma Y,Eckelman WC

doi

10.1016/s0969-8051(00)00111-6

keywords:

subject

Has Abstract

pub_date

2000-07-01 00:00:00

pages

457-62

issue

5

eissn

0969-8051

issn

1872-9614

pii

S0969-8051(00)00111-6

journal_volume

27

pub_type

杂志文章,评审

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