Tremor-producing activity and concentration in brain were determined in mice for 4 harmala and 5 iboga alkaloids. All compounds were active, however, harmalol only after intracerebral injection. Kinetics of evasion from brain were first-order functions with most drugs, but revealed 2 compartments for harmalol and 3 for ibogaline. Tremor-producing activity was much more influenced by chemical structure than by lipid solubility. This points to specific receptors for indole compounds in tremorigenic brain structures.
An ethanol total extract of the roots of Valeriana officinalis L. in doses equivalent to 0.5–800 mg valerian root/kg b.w.i.p. was tested in male mice for possible neuropharmacological efficacy and in this respect compared with diazepam and haloperidol. The extract did not modify spontaneous motility, nociception or body temperature, and did not produce palpebral ptosis. However, it was anticonvulsant against picrotoxin (but not pentetrazol and harman) with an ED50 between 4.5 and 6 mg/kg and it prolonged thiopental anaesthesia. After fractionation of the crude extract, the antipicrotoxin activity was present mainly in the methylene chloride fraction (ED50=0.25 mg/kg). Pure valerenic acid (12.5 mg/kg b.w.i.p.) also exerted an antipicrotoxin effect.
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