Arylacetamide-derived fluorescent probes: synthesis, biological evaluation, and direct fluorescent labeling of kappa opioid receptors in mouse microglial cells.

@article{Chang1996ArylacetamidederivedFP,
  title={Arylacetamide-derived fluorescent probes: synthesis, biological evaluation, and direct fluorescent labeling of kappa opioid receptors in mouse microglial cells.},
  author={Andy C-M. Chang and Chun Cheih Chao and Akihiro Takemori and Genya Gekker and Shirley X Hu and Phillip K. Peterson and Philip S. Portoghese},
  journal={Journal of medicinal chemistry},
  year={1996},
  volume={39 8},
  pages={1729-35}
}
Fluorescein isothiocyanate isomer I (FITC-I) conjugates of 2-(3,4-dichlorophenyl)-N-methyl-N-[1-(3- or 4-aminophenyl)-2-(1-pyrrolidinyl)ethyl]acetamide (10 and 14) were prepared either without or with an intervening mono-, di-, or tetraglycyl linker. The 3-substituted fluorescent probes (2-5) were found to retain potent agonist activity in smooth muscle preparations as well as high kappa receptor affinity and selectivity in receptor binding assays. The 4-substituted series (6-9) were… CONTINUE READING

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