Differential effects of sedative and anticonvulsant barbiturates on specific [3H]GABA binding to membrane preparations from rat brain cortex

Whittle, Susan R.; Turner, Anthony J.

doi:10.1016/0006-2952(82)90260-x

Cited by 61 publications

(28 citation statements)

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“…did not alter the concentration of GABA in the (Harrison & Simmonds, 1983) and cultured rat spinal cord neurones (Hedlund et al, 1987 (Whittle & Turner, 1982). By analogy with these barbiturates it would seem likely that the interaction of chlormethiazole with the [35S]-TBPS binding site may relate to its sedative effect.…”

Section: Discussionmentioning

confidence: 99%

“…Barbiturates and some related compounds have been shown to interact with the TBPS/picrotoxinin binding site labelled by [35S]-TBPS in brain membranes (Squires et al, 1983). In addition, sedative barbiturates will potentiate the binding of [3H]-muscimol and [3H]-flunitrazepam to the GABAA-receptor (Leeb-Lundberg et al, 1980;Whittle & Turner, 1982;Thyagarajan et al, 1983;Lohse et al, 1987).…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

The modulation by chlormethiazole of the GABA_A‐receptor complex in rat brain

Cross¹,

Jm²,

Tn³

et al. 1989

British J Pharmacology

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

The modulation by chlormethiazole of the GABA_A‐receptor complex in rat brain

Cross¹,

Jm²,

Tn³

et al. 1989

British J Pharmacology

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“…Their most remarkable action is on the central nervous system. They are extensively used for producing effects ranging from mild sedation to anaesthesia [17][18][19][20][21] as anticonvulsants, anxiolytics, sedative, and antiepileptic agents, as well as antitumoral agents [22][23][24][25][26]. They have found a prominent 2 Journal of Chemistry place in pharmaceutical industry because of their biochemical effects on calcium, acetylcholine, biogenic amines, glutamate, aspartate, and gamma-aminobutyric acid [27].…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Characterization, and Tautomerism of 1,3-Dimethyl Pyrimidine-2,4,6-Trione s-Triazinyl Hydrazine/Hydrazone Derivatives

Sharma

Jad

Siddiqui

et al. 2017

Journal of Chemistry

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1,3,5-Triazines and pyrimidine-2,4,6-triones belong to that class of compounds which are well known in literature for possessing wide range of biological activities. Here, we report a new family of compounds that encompasses these two structures. The union of both heterocycles was carried out through a hydrazone moiety incorporated into an acetyl group at the position 5 of 1,3-dimethyl pyrimidine derivative. The synthetic strategy adopted allowed the preparation of the target compounds with excellent yields and good purities. The synthesized compounds were well characterized by NMR (1H and 13C), HRMS, and elemental analysis. Furthermore, the tautomerism of enhydrazine versus hydrazone has also been studied.

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“…Commonly, they are used to treat anxiety, insomnia, seizure disorders, migraine headaches and in surgery as general anesthetics, anticonvulsants, and anxiolytics [1][2][3][4][5][6][7]. Barbiturates analogs deep coma.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Crystal Structure and DFT Studies of 1,3-Dimethyl-5-propionylpyrimidine-2,4,6(1H,3H,5H)-trione

et al. 2017

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Novel 1,3-Dimethyl-5-propionylpyrimidine-2,4,6(1H,3H,5H)-trione was synthesized and recrystallized from ethanol. The compound was characterized by 1 H NMR, 13 C NMR in CDCl 3 , DMSO-d 6 and acetone-d 6 , elemental analysis and X-ray diffraction. The NMR data observed that the title compound exists in the enol tautomer rather than keto, and it stabilized by strong H-bond as observed form the NMR data at different temperatures. Theoretical calculations (DFT) were carried out using Gaussian09 program package and B3LYP correlation function. Full geometry optimization of the keto and enol forms were carried out using 6-311G++(d,p) basis set. The structure and energy of the transition state between these two tautomers were calculated. The frontier orbital energy and atomic net atomic charges of the tautomers were presented. The experimental results of the title compound have been compared with the theoretical results and it was found that the experimental data are in a good agreement with the calculated values. The transition state calculations also support the stability of enol form compared to keto form at room temperature.

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Differential effects of sedative and anticonvulsant barbiturates on specific [3H]GABA binding to membrane preparations from rat brain cortex

Cited by 61 publications

References 28 publications

The modulation by chlormethiazole of the GABA_A‐receptor complex in rat brain

The modulation by chlormethiazole of the GABA_A‐receptor complex in rat brain

Synthesis, Characterization, and Tautomerism of 1,3-Dimethyl Pyrimidine-2,4,6-Trione s-Triazinyl Hydrazine/Hydrazone Derivatives

Synthesis, Crystal Structure and DFT Studies of 1,3-Dimethyl-5-propionylpyrimidine-2,4,6(1H,3H,5H)-trione

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Differential effects of sedative and anticonvulsant barbiturates on specific [3H]GABA binding to membrane preparations from rat brain cortex

Cited by 61 publications

References 28 publications

The modulation by chlormethiazole of the GABAA‐receptor complex in rat brain

The modulation by chlormethiazole of the GABAA‐receptor complex in rat brain

Synthesis, Characterization, and Tautomerism of 1,3-Dimethyl Pyrimidine-2,4,6-Trione s-Triazinyl Hydrazine/Hydrazone Derivatives

Synthesis, Crystal Structure and DFT Studies of 1,3-Dimethyl-5-propionylpyrimidine-2,4,6(1H,3H,5H)-trione

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The modulation by chlormethiazole of the GABA_A‐receptor complex in rat brain

The modulation by chlormethiazole of the GABA_A‐receptor complex in rat brain