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Small molecule drug	1

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5-HT1A receptor x 5-HT2C receptor	1

The effects of i.v. injected adrenaline (2 μg./kg./min.) on the frequency and force of cardiac contraction, arterial pressure, and on the flow, O saturation, CO2 level, and NH3 level of coronary venous blood were determined before and after injection of atropine (0.2 mg./kg.) into chloralosed dogs.Adrenaline caused a reflex bradycardia and a 73% increase in contractile force in the presence of functional cardioregulatory innervation but produced tachycardia and a 108% increase in contractile force in its absence (in atropine-treated dogs).In nonatropinized dogs, the coronary venous blood O saturation was increased 81% after injection of adrenaline, although the CO2 and NH3 levels were not significantly altered, while in atropinized dogs the O saturation was not significantly increased but blood CO2 and NH3 levels were increased by 10 and 22%, resp.However, injection of adrenaline before and after atropine caused similar increases in coronary blood flow (73 and 68%, resp.) even though adrenaline caused the above different metabolic effects under these 2 conditions.The metabolic variations are therefore not responsible for the coronary-dilator effect of adrenaline but the latter is probably a direct vasodilator effect.15 references.

Farmaco, Edizione Pratica

Pharmacodynamic properties of 7-chloro-1,3-dihydro-3-hemisuccinyloxy-5-phenyl-2H-1,4-benzodiazepin-2-one

Author: Torrielli, M. V. ; Duchene-Marullaz, Pierre ; Lakatos, Claire ; De Marchi, Franco

The oral, i.p., and i.v. LD50 values of the title compound (I) were 1148, 375, and 285 mg./kg., resp., in mice and this compound is therefore less toxic than the reference compound, chlordiazepoxide (II).Administration of a 25 mg./kg. dose to mice reduced the aggression or flight reactions but did not greatly reduce spontaneous activity.In various behavior tests, I was more effective than II in reducing agility and it also caused incoordination (due to muscle hypotonus), but neither compound altered initiative activity as measured by the evasion test.I (doses >12.5 mg./kg.) slightly reduced the spontaneous activity, but to a lesser extent than II.I had anticonvulsant activity which was 13- and 3-fold greater than that of II against pentetrazole and strychnine, resp., but equal activity was shown towards convulsions in mice given tremorine.I, given orally (6.25, 12.5, or 25 mg./kg.), was more effective than II in potentiating the activity of a nonsedative dose of pentobarbital (i.p. injection of 12.5 mg./kg.).I had no significant general pharmacol. effects when given i.v. to cats and rats (doses up to 40 and 16 mg./kg., resp.) or by gastric tube to dogs (40 mg./kg.) or when given for 90 days to rats at 1/20th of the oral and i.p. LD50 values.I (20 or 40 mg./kg.) did not alter the responses to adrenaline, noradrenaline, carotid occlusion, or vagal stimulation when given by gastric tube to dogs.

Comptes Rendus des Seances de la Societe de Biologie et de Ses Filiales

Duration of the vagolytic action of atropine

Author: DucheneMarullaz, P. ; Vacher, J. ; Valensi, F.

Dogs wearing an attached cardiotachymetric device were injected intravenously with atropine, 0.2 mg./kg.The vagolytic (cardioaccelerator) action was complete for 10 min. only, then declined, and practically disappeared after 2.5 hrs.

100 Deals associated with Centre européen de recherches Mauvernay

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100 Translational Medicine associated with Centre européen de recherches Mauvernay

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Pipeline

Pipeline Snapshot as of 24 Nov 2024

The statistics for drugs in the Pipeline is the current organization and its subsidiaries are counted as organizations,Early Phase 1 is incorporated into Phase 1, Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3

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