Literature DB >> 1185595

A comparison of the potencies of a series of barbiturates at the neuromuscular junction and on the central nervous system.

S Lee-Son, B E Waud, D R Waud.   

Abstract

The ability of a series of barbiturates to depress the depolarizing action of carbachol at the end-plate of guinea-pig lumbrical muscle was studied. The compounds studied were: amorbarbital, aprobarbital, barbital, barbituric acid, butabarbital, butalbital, dimethylbutylethyl barbituric acid, hexobarbital, mephobarbitak, secobarbital, thiamylal, and thiopental. The depressant activity was sensitive to small changes in structure of the compounds strongly suggesting that a specific receptor site was involved in the interaction of the drug with the tissue. The observed relative potencies on the motor end-plate were compared with their anesthetic potencies assayed on tadpoles. The two potencies went hand-in-hand for all the compounds studied, including the convulsant member of the series.

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Year:  1975        PMID: 1185595

Source DB:  PubMed          Journal:  J Pharmacol Exp Ther        ISSN: 0022-3565            Impact factor:   4.030


  7 in total

1.  Allyl m-trifluoromethyldiazirine mephobarbital: an unusually potent enantioselective and photoreactive barbiturate general anesthetic.

Authors:  Pavel Y Savechenkov; Xi Zhang; David C Chiara; Deirdre S Stewart; Rile Ge; Xiaojuan Zhou; Douglas E Raines; Jonathan B Cohen; Stuart A Forman; Keith W Miller; Karol S Bruzik
Journal:  J Med Chem       Date:  2012-07-17       Impact factor: 7.446

Review 2.  Mapping General Anesthetic Sites in Heteromeric γ-Aminobutyric Acid Type A Receptors Reveals a Potential For Targeting Receptor Subtypes.

Authors:  Stuart A Forman; Keith W Miller
Journal:  Anesth Analg       Date:  2016-11       Impact factor: 5.108

3.  Mechanisms of barbiturate inhibition of acetylcholine receptor channels.

Authors:  J P Dilger; R Boguslavsky; M Barann; T Katz; A M Vidal
Journal:  J Gen Physiol       Date:  1997-03       Impact factor: 4.086

4.  Specificity of intersubunit general anesthetic-binding sites in the transmembrane domain of the human α1β3γ2 γ-aminobutyric acid type A (GABAA) receptor.

Authors:  David C Chiara; Selwyn S Jayakar; Xiaojuan Zhou; Xi Zhang; Pavel Y Savechenkov; Karol S Bruzik; Keith W Miller; Jonathan B Cohen
Journal:  J Biol Chem       Date:  2013-05-15       Impact factor: 5.157

5.  Inhibition of the nicotinic acetylcholine receptor by barbiturates and by procaine: do they act at different sites?

Authors:  C S Yost; B A Dodson
Journal:  Cell Mol Neurobiol       Date:  1993-04       Impact factor: 5.046

6.  High-throughput Screening in Larval Zebrafish Identifies Novel Potent Sedative-hypnotics.

Authors:  Xiaoxuan Yang; Youssef Jounaidi; Jennifer B Dai; Francisco Marte-Oquendo; Elizabeth S Halpin; Lauren E Brown; Richard Trilles; Wenqing Xu; Renee Daigle; Buwei Yu; Scott E Schaus; John A Porco; Stuart A Forman
Journal:  Anesthesiology       Date:  2018-09       Impact factor: 7.892

7.  Relative potencies for barbiturate binding to the Torpedo acetylcholine receptor.

Authors:  B A Dodson; R R Urh; K W Miller
Journal:  Br J Pharmacol       Date:  1990-11       Impact factor: 8.739

  7 in total

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