Effect of desmethyldiazepam and chlordesmethyldiazepam on 3′,5′-cyclic guanosine monophosphate levels in rat cerebellum

  title={Effect of desmethyldiazepam and chlordesmethyldiazepam on 3′,5′-cyclic guanosine monophosphate levels in rat cerebellum},
  author={Stefano Govoni and Paola Fresia and PierFranco Spano and Marco Trabucchi},
Three different benzodiazepines (diazepam, its pharmacologically active metabolite desmethyldiazepam, and the derivative chlordesmethyldiazepam) have been compared in our study for their effects on 3′,5′-guanosine monophosphate (cGMP) cerebellar levels. Desmethyldiazepam and chlordesmethyldiazepam are several-fold more potent that diazepam in decreasing rat cyclic cGMP cerebellar concentrations. None of the three drugs induces detectable changes of cerebellar cyclic 3′,5′-adenosine… 

Anticonvulsant action of diazepam in mice pretreated with caffeine.

First spike, clonic and tonic convulsions induced by PTZ were readily recognized from the EEG recording coupled with EMG recording, and these anticonvulsive effects of diazepam were also observed when PTZ-induced Convulsions were potentiated with caffeine, except for clonic convulsion which was not suppressed with diazepAM.

Spontaneous activity of mollusk neurons as a model for sampling of anticonvulsants

During the study of the effect of medic ina l p repa ra t ions on the whole animal o r g a n i s m by means of conventional pha rmaco log ica l methods, i t is usual ly imposs ib le to show the

The effect of naloxone on cerebellar cGMP content

The results support the assumption proposed by other authors that naloxone exerts GABA antagonistic effects aside from the potent opiate receptor antagonistic activity.



Interactions betweeen γ aminobutyric acid and guanosine cyclic 3',5' monophosphate in rat cerebellum

Of the three drugs—aminooxyacetic acid, hydrazine sulfate, and hydroxylamine—which increase cerebellar concentrations of γ-aminobutyric acid (GABA), the first two inhibited the increase in cGMP concentration elicited by cold exposure, and the inhibition of the increment in Cerebellar cG MP elicitedBy cold correlated with the extent of the increased in cerebellary GABA concentrations.

Radioimmunoassay for cyclic nucleotides. 3. Effect of ischemia, changes during development and regional distribution of adenosine 3',5'-monophosphate and guanosine 3',5'-monophosphate in mouse brain.

The changes in cGMP levels between 7 days and adulthood were quite unlike those of cAMP, and there was no change in forebrain c GMP, brain stem cG MP increased 2-fold, and in cerebellum cGmp rose dramatically, to a level 13 times that at 7 days.

Plasma concentrations of diazepam and of its metabolite N‐desmethyldiazepam in relation to anxiolytic effect

The results suggest that the degree of the diazepam effect is directly proportional to plasma concentrations and reCiprocal clearance values of diazepAM and N‐desmethyldiazepam.

Effects and plasma levels of N-desmethyldiazepam after oral administration in normal volunteers

  • H. Dasberg
  • Psychology, Medicine
  • 2004
Results showed that steady state plasma levels were reached on the 5th day; that N-desmethyldiazepam, considering its lower clearance rates, is a longer acting drug than diazepam; that both substances induce hypnosedative effects, mood changes, and somatic disturbances and facilitate sexual behaviour in normals.