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.
Two ethanolic dry extracts from the herb Chelidonium majus L. with a defined content of the main alkaloids (chelidonine, protopine, and coptisisine) and the alkaloids themselves were studied in three different antispasmodic test models on isolated ileum of guinea-pigs. In the BaCl2-stimulated ileum, chelidonine and protopine exhibited the known papaverine-like musculotropic action, whereas coptisine (up to 3.0 x 10(-5) g/ml) was ineffective in this model. Both extracts were active with 53.5% and 49.0% relaxation at 5 x 10(-4) g/ml. The carbachol and the electric field stimulated contractions were antagonized by all three alkaloids. Coptisine showed competitive antagonist behaviour with a pA2 value of 5.95. Chelidonine and protopine exhibited a certain degree of non-competitive antagonism. In the electric field the antagonist activities decreased in the order protopine > coptisine > chelidonine. The concentrations of the chelidonium herb extracts for 50% inhibition of the carbachol and electrical field induced spasms were in the range of 2.5 to 5 x 10(-4) g/ml.
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