Correlation of 3H-Rolipram Binding to a Cerebral cAMP Phosphodiesterase with Antidepressant Activity
Rolipram, which has a proven effectiveness as an antidepressant in the clinic (Eckmann et al., 1988) indirectly enhances noradrenergic transmission. The phosphodiesterase (PDE) inhibitory action of rolipram has been known for several years, yet the high selectivity and potency of cAMP PDE inhibition which had been suggested from behavioural experiments (Wachtel, 1982) has been confirmed only recently after partial purification of a rolipram-sensitive PDE isozyme (RsPDE) by affinity chromatography (Schneider et al., 1988). 3H-rolipram binds specifically to brain protein constituents (Schneider et al., 1986), which may allow an alternative access to the target site of rolipram’s action.
KeywordsAntidepressant Activity Head Twitch Mouse Forebrain Monoamine Receptor Glass Fiber Disc
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