TY - JOUR
T1 - 14-desoxy analogues of naltrindole and 7-spiroindanyloxymorphone
T2 - The role of the 14-hyroxy group at δ opioid receptors
AU - Kshirsagar, Tushar A.
AU - Fang, Xinqin
AU - Portoghese, Philip S.
PY - 1998/7/2
Y1 - 1998/7/2
N2 - The 14-hydroxy group is known to increase the antagonist potency of μ- selective opioid ligands. To investigate the role of this group at the δ opioid receptor, the 14-desoxy analogues (7 and 9) of the δ-selective ligands, naltrindole (1, NT1) and spiroindanyloxymorphone (2, SIOM), have been synthesized and tested. The in vitro pharmacologic activities of 7 and 9 suggest that the 14-hydroxy group plays an important role in determining the δ selectivity and potency of NT1 and SIOM.
AB - The 14-hydroxy group is known to increase the antagonist potency of μ- selective opioid ligands. To investigate the role of this group at the δ opioid receptor, the 14-desoxy analogues (7 and 9) of the δ-selective ligands, naltrindole (1, NT1) and spiroindanyloxymorphone (2, SIOM), have been synthesized and tested. The in vitro pharmacologic activities of 7 and 9 suggest that the 14-hydroxy group plays an important role in determining the δ selectivity and potency of NT1 and SIOM.
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U2 - 10.1021/jm980209b
DO - 10.1021/jm980209b
M3 - Article
C2 - 9651172
AN - SCOPUS:0032474783
SN - 0022-2623
VL - 41
SP - 2657
EP - 2660
JO - Journal of medicinal chemistry
JF - Journal of medicinal chemistry
IS - 14
ER -