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This study searched for polymorphic sites in the murine μ-, δ- and κ-opioid receptors that presumably influence pain perception. We employed two mouse lines divergently bred for high (HA, high analgesia line) and low (LA, low analgesia line) swim stress-induced analgesia (SSIA). These mouse lines differ substantially in pain sensitivity, measured as hind paw withdrawal latency in the hot-plate test...
Alcoholism is a complex disorder, still not fully understood, in which environmental and inherited risk factors play essential roles. Of particular importance may be chronic exposure to stress thought to increase preference for ethanol in genetically susceptible individuals. Animal and human data suggest that the opioid system may be involved in the development of alcohol dependence. We studied the...
The synthesis of tryptophan analogs is reported in which the conformation has been constrained by formation of a seven-membered lactam. Boc-protected 2′-formyl tryptophan was obtained by SeO 2 oxidation of Boc-tetrahydro-β-carboline-3-carboxylic acid. Reductive amination was performed with a variety of amines and amino acid esters using sodium cyanoborohydride, followed by ring closure to...
New analogues of deltorphin I (DT I), in which the phenylalanine residue in position 3 is substituted with amphiphilic α,α-disubstituted amino acid enantiomers, (R) and (S)-α-hydroxymethylnaphtylalanine, were synthesized and tested for μ and δ opioid receptor affinity and selectivity. Although both analogues have lower affinity to δ receptors than DT I, they both expressed specificity to δreceptors.
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