Literature DB >> 32151384

Neuroactive steroids alphaxalone and CDNC24 are effective hypnotics and potentiators of GABAA currents, but are not neurotoxic to the developing rat brain.

Vesna Tesic1, Srdjan M Joksimovic1, Nidia Quillinan2, Kathiresan Krishnan3, Douglas F Covey4, Slobodan M Todorovic2, Vesna Jevtovic-Todorovic5.   

Abstract

BACKGROUND: The most currently used general anaesthetics are potent potentiators of γ-aminobutyric acid A (GABAA) receptors and are invariably neurotoxic during the early stages of brain development in preclinical animal models. As causality between GABAA potentiation and anaesthetic-induced developmental neurotoxicity has not been established, the question remains whether GABAergic activity is crucial for promoting/enhancing neurotoxicity. Using the neurosteroid analogue, (3α,5α)-3-hydroxy-13,24-cyclo-18,21-dinorchol-22-en-24-ol (CDNC24), which potentiates recombinant GABAA receptors, we examined whether this potentiation is the driving force in inducing neurotoxicity during development.
METHODS: The neurotoxic potential of CDNC24 was examined vis-à-vis propofol (2,6-diisopropylphenol) and alphaxalone (5α-pregnan-3α-ol-11,20-dione) at the peak of rat synaptogenesis. In addition to the morphological neurotoxicity studies of the subiculum and medial prefrontal cortex (mPFC), we assessed the extra-, pre-, and postsynaptic effects of these agents on GABAergic neurotransmission in acute subicular slices from rat pups.
RESULTS: CDNC24, like alphaxalone and propofol, caused dose-dependent hypnosis in vivo, with a higher therapeutic index. CDNC24 and alphaxalone, unlike propofol, did not cause developmental neuroapoptosis in the subiculum and mPFC. Propofol potentiated post- and extrasynaptic GABAA currents as evidenced by increased spontaneous inhibitory postsynaptic current (sIPSC) decay time and prominent tonic currents, respectively. CDNC24 and alphaxalone had a similar postsynaptic effect, but also displayed a strong presynaptic effect as evidenced by decreased frequency of sIPSCs and induced moderate tonic currents.
CONCLUSIONS: The lack of neurotoxicity of CDNC24 and alphaxalone may be at least partly related to suppression of presynaptic GABA release in the developing brain.
Copyright © 2020 British Journal of Anaesthesia. Published by Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  general anaesthetic; prefrontal cortex; presynaptic; subiculum; synaptic transmission; synaptogenesis

Mesh:

Substances:

Year:  2020        PMID: 32151384      PMCID: PMC7222221          DOI: 10.1016/j.bja.2020.01.013

Source DB:  PubMed          Journal:  Br J Anaesth        ISSN: 0007-0912            Impact factor:   9.166


  40 in total

Review 1.  Which molecular targets are most relevant to general anaesthesia?

Authors:  N P Franks; W R Lieb
Journal:  Toxicol Lett       Date:  1998-11-23       Impact factor: 4.372

Review 2.  Spontaneous neurotransmission: an independent pathway for neuronal signaling?

Authors:  Ege T Kavalali; Chihye Chung; Mikhail Khvotchev; Jeremy Leitz; Elena Nosyreva; Jesica Raingo; Denise M O Ramirez
Journal:  Physiology (Bethesda)       Date:  2011-02

Review 3.  Exposure of Developing Brain to General Anesthesia: What Is the Animal Evidence?

Authors:  Vesna Jevtovic-Todorovic
Journal:  Anesthesiology       Date:  2018-04       Impact factor: 7.892

4.  Modulation of GABAA receptor activity by alphaxalone.

Authors:  G A Cottrell; J J Lambert; J A Peters
Journal:  Br J Pharmacol       Date:  1987-03       Impact factor: 8.739

5.  Quantal analysis of inhibitory synaptic transmission in the dentate gyrus of rat hippocampal slices: a patch-clamp study.

Authors:  F A Edwards; A Konnerth; B Sakmann
Journal:  J Physiol       Date:  1990-11       Impact factor: 5.182

6.  Potential Adverse Effects of Prolonged Sevoflurane Exposure on Developing Monkey Brain: From Abnormal Lipid Metabolism to Neuronal Damage.

Authors:  Fang Liu; Shuo W Rainosek; Jessica L Frisch-Daiello; Tucker A Patterson; Merle G Paule; William Slikker; Cheng Wang; Xianlin Han
Journal:  Toxicol Sci       Date:  2015-07-23       Impact factor: 4.849

Review 7.  The role of medial prefrontal cortex in memory and decision making.

Authors:  David R Euston; Aaron J Gruber; Bruce L McNaughton
Journal:  Neuron       Date:  2012-12-20       Impact factor: 17.173

8.  Propofol-induced apoptosis of neurones and oligodendrocytes in fetal and neonatal rhesus macaque brain.

Authors:  C Creeley; K Dikranian; G Dissen; L Martin; J Olney; A Brambrink
Journal:  Br J Anaesth       Date:  2013-06       Impact factor: 9.166

9.  Clinical anesthesia causes permanent damage to the fetal guinea pig brain.

Authors:  Sabina Rizzi; Lisa B Carter; Carlo Ori; Vesna Jevtovic-Todorovic
Journal:  Brain Pathol       Date:  2008-01-29       Impact factor: 6.508

Review 10.  Pathophysiological power of improper tonic GABA(A) conductances in mature and immature models.

Authors:  Kiyoshi Egawa; Atsuo Fukuda
Journal:  Front Neural Circuits       Date:  2013-10-24       Impact factor: 3.492

View more
  6 in total

Review 1.  Synthetic neuroactive steroids as new sedatives and anaesthetics: Back to the future.

Authors:  Francesca M Manzella; Douglas F Covey; Vesna Jevtovic-Todorovic; Slobodan M Todorovic
Journal:  J Neuroendocrinol       Date:  2022-01-10       Impact factor: 3.627

2.  Preemptive Analgesic Effect of Intrathecal Applications of Neuroactive Steroids in a Rodent Model of Post-Surgical Pain: Evidence for the Role of T-Type Calcium Channels.

Authors:  Quy L Tat; Srdjan M Joksimovic; Kathiresan Krishnan; Douglas F Covey; Slobodan M Todorovic; Vesna Jevtovic-Todorovic
Journal:  Cells       Date:  2020-12-12       Impact factor: 6.600

3.  Edaravone Alleviated Propofol-Induced Neurotoxicity in Developing Hippocampus by mBDNF/TrkB/PI3K Pathway.

Authors:  Yangliang Yang; Jing Yi; Mengzhi Pan; Baoji Hu; Hongwei Duan
Journal:  Drug Des Devel Ther       Date:  2021-03-30       Impact factor: 4.162

Review 4.  Do We Have Viable Protective Strategies against Anesthesia-Induced Developmental Neurotoxicity?

Authors:  Nemanja Useinovic; Stefan Maksimovic; Michelle Near; Nidia Quillinan; Vesna Jevtovic-Todorovic
Journal:  Int J Mol Sci       Date:  2022-01-20       Impact factor: 5.923

Review 5.  General Anesthesia and the Young Brain: The Importance of Novel Strategies with Alternate Mechanisms of Action.

Authors:  Stefan Maksimovic; Nemanja Useinovic; Nidia Quillinan; Douglas F Covey; Slobodan M Todorovic; Vesna Jevtovic-Todorovic
Journal:  Int J Mol Sci       Date:  2022-02-08       Impact factor: 5.923

6.  An Integrative Bioinformatics Analysis of the Potential Mechanisms Involved in Propofol Affecting Hippocampal Neuronal Cells.

Authors:  Zhao Zhuang; Dajiang Li; Mengmeng Jiang; Ye Wang; Qianqian Cao; Shenfeng Li; Ruixue Luan; Lina Sun; Shoushi Wang
Journal:  Comput Intell Neurosci       Date:  2022-04-26
  6 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.