Discovery of a Nociceptin Receptor Antagonist
J ournal of Medicinal Chemistry, 1998, Vol. 41, No. 18 3365
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sponse; apparent affinities of antagonists are given in terms
of pA2 ) the negative logarithm to base 10 of the molar
concentration of an antagonist that makes it necessary to
double the concentration of agonist needed to elicit the original
submaximal response. Antagonist apparent affinities have
been evaluated using the Gaddum Schild equation, pA2
-log(CR - 1/[antagonist]) assuming a slope value equal to
)
unity.
Ack n ow led gm en t. We thank Dr. M. Remelli for
chiral HPLC analysis (not mentioned in the text). This
work was supported by the Italian Ministry of the
University (40% and 60% grants).
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