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The purpose of the present study was to characterize the 5-HT autoreceptor in the lumbar spinal cord of the rat. The effect of selective 5-HT1A and 5-HT1B agonists on K+-evoked release of [3H]5-HT and the binding of [3H]5-HT were examined. The 5-HT1B compounds, mCPP and quipazine were more potent than exogenous 5-HT at decreasing K+-evoked release of [3H]5-HT in slices of spinal cord. The pEC40 values of 5-HT agonists tested, determined from release assays, significantly correlated with the relative affinities (pKD's) of these compounds for the binding of [3H]5-HT to the 5-HT1B receptor subtype in the presence of 2 microM 8-OHDPAT, as determined from radioligand binding studies (r = 0.98, P = 0.003). Conversely, the potencies of the 5-HT1A agonists 5-MeODMT and 8-OHDPAT, at the 5-HT autoreceptor, were negatively correlated (r = -0.77, P less than 0.10) with their potencies at displacing [3H]5-HT from the 5-HT1A subsite (binding of [3H]5-HT in the presence of 1 microM mCPP). Thus, the 5-HT autoreceptor in spinal cord appears to bear a significant pharmacological similarity to the 5-HT1B binding site. Further testing of the present results requires the development of new 5-HT1 agonists which are selective (1000-fold difference) for the 5-HT1A and 5-HT1B subsites.
R M Murphy, and
F P Zemlan
January 1988,
European journal of pharmacology,
R M Murphy, and
F P Zemlan
November 1981,
European journal of pharmacology,
R M Murphy, and
F P Zemlan
June 1999,
European journal of pharmacology,
R M Murphy, and
F P Zemlan
November 1995,
British journal of pharmacology,
R M Murphy, and
F P Zemlan
December 1998,
Annals of the New York Academy of Sciences,
R M Murphy, and
F P Zemlan
September 2009,
Archives of orthopaedic and trauma surgery,
R M Murphy, and
F P Zemlan
November 1989,
Brain research,
R M Murphy, and
F P Zemlan
May 1991,
Brain research,
R M Murphy, and
F P Zemlan
April 2009,
Journal of neurotrauma,
R M Murphy, and
F P Zemlan
July 1998,
Behavioural pharmacology,
