Coumarin is a natural compound well known for its phytotoxic potential. In the search for new herbicidal compounds to manage weeds, three synthetic derivatives bearing the coumarin scaffold (1-3), synthesized by a carbonylative organometallic approach, were in vitro assayed on germination and root growth of two noxious weeds, Amaranthus retroflexus and Echinochloa crus-galli. Moreover, the synt...

We have studied the dose-response relationships for neostigmine and edrophonium during antagonism of neuromuscular block induced by mivacurium chloride. Sixty-four ASA group I or II adults were given mivacurium 0.15 mg kg-1 during fentanyl-thiopentone-nitrous oxide-isoflurane anaesthesia. Train-of-four stimulation (TOF) was applied to the ulnar nerve every 10 s, and the force of contraction of ...

We have developed an assay where the potency of retinoids in retinoic acid receptor (RAR) mediated transcriptional activation can be rapidly evaluated. In this assay hRAR-alpha, hRAR-beta and hRAR-gamma were expressed in CV-1 cells together with a reporter gene containing a retinoic acid responsive element (TRE3-tk-CAT). Concentrations required to obtain half-maximum induction (ED50) of CAT-act...

By using, as a model, cultured testicular immature Sertoli cells, the action of tumor necrosis factor-alpha (TNF alpha) and the site of action of the cytokine on lactate production were studied. TNF alpha stimulated in a time- and dose-dependent manner (with an ED50 of 0.1 nM) Sertoli cell lactate production. Two major sites involved in TNF alpha action were identified. Firstly, TNF alpha was s...

The laser-induced retinal injury thresholds for repetitive-pulse exposures to 100-μs-duration pulses at a wavelength of 532 nm have been determined for exposures of up to 1000 pulses in an in vivo model. The ED50 was measured for pulse repetition frequencies of 50 and 1000 Hz. Exposures to collimated beams producing a minimal retinal beam spot and to divergent beams producing a 100-μm-diameter ...

Aminophylline (50-100 mg/kg) and strychnine (0.125-0.5 mg/kg) significantly raised the ED50 values of LY 300164 against maximal electroshock in mice, from 4 to 8 mg/kg (aminophylline 100 mg/kg) and from 3.6 to 11.5 mg/kg (strychnine 0.5 mg/kg). Also, aminophylline (25-50 mg/kg) and strychnine (0.125-0.25 mg/kg) increased the ED50 value of lamotrigine in this test, for instance from 5.5 to 8.0 m...

in order to study the effect of soil nitrogen content and water hardness on glyphosate efficacy on common lambsquarter (chenopodium album l.) and redroot pigweed (amaranthus retroflexus l.) control, an experiment was carried out as a completely randomized design in a factorial arrangement with three replications. experimental treatments were included soil nitrogen content (18, 50, 90, 200 and 3...

Considerable interest has been focused on the triazole structure, which has been known to possess a broad spectrum of biological activities such as antitumor, anti-inflammatory, antimicrobial, antiviral, and anticonvulsant activities. Before this, several heterocyclic compounds containing triazole were synthesized that had shown considerable anticonvulsant activity. As part of our continuous re...

Introduction: The use of the pharmacophoric approach is a promising direction for modifying chemical structure 2-propylpentanoic (valproic) acid in order to obtain new drugs.
 Materials and methods: In experiments on mice, acute toxicity, neurotoxicity, antiepileptic activity analgesic effect N-(5-ethyl-1,3,4-thiadiazol-2-yl)-2-propylpentanamide (valprazolamide) were evaluated. LD50 was de...

The compound, LY368975 ((R)-thionisoxetine) is a potent and selective inhibitor of the norepinephrine (NE) reuptake site. We evaluated the in vivo properties of LY368975 in various animal models. In mice, LY368975 prevented heart NE depletion by 6-hydroxydopamine with an ED50 of 1.22 mg/kg. In rats, orally administered LY368975 inhibited 3H-NE uptake into hypothalamic synaptosomes ex vivo with ...