The 1‐(2‐hydroxy‐1‐phenylethyl)‐imidazole derivative Hoe 249 has a profile which suggests the compound is a promising candidate for clinical evaluation as an antidepressant drug. In pharmacological tests commonly considered predictive of antidepressant activity, e.g., reserpine‐ and tetrabenazine‐antagonism, reversal of oxotremorine‐ and apomorphine‐induced hypothermia, and potentiation of yohimbine toxicity, Hoe 249 is equipotent to nomifensine, but does not meet excitation and stereotypic behavior in a comparable dose range. Hoe 249 shows weak anticonvulsant activity against pentylenetetrazole‐induced seizures and it causes a slight dose‐dependent prolongation of hexobarbital narcosis. Biochemical studies characterize Hoe 249 as an inhibitor of synaptosomal dopamine and norepinephrine uptake, whereas serotonin uptake is not influenced.
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Alpermann et al. (1992) studied this question.
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