Abstract:
:Allopregnanolone (AP) is an endogenous neurosteroid. It modulates the effect of γ-amino-butyric acid (GABA) on the GABA type A (GABAA) receptor, which leads to increased receptor activity. Since the GABA-system is mainly inhibitory, increased AP activity leads to modulation of neuronal activity. In vitro studies of GABAA receptor activity and in vivo animal studies of sedation have shown that AP-induced effects can be inhibited by another endogenous steroid, namely isoallopregnanolone (ISO). In this study we investigated if ISO can antagonize AP-induced effects in healthy female volunteers, via measurements of saccadic eye velocity (SEV) and self-rated sedation. With a single-blind cross-over design, 12 women were studied on three separate occasions; given AP alone or AP in combination with one of two ISO doses. Congruent with previous reports, AP administration decreased SEV and induced sedation and these effects were diminished by simultaneous ISO administration. Also, the ISO effect modulation was seemingly stronger for SEV than for sedation. These effects were observed already at an ISO dose exposure that was approximately half of that of AP. In conclusion, ISO antagonized AP-induced decrease in SEV and self-reported sedation, probably in a non-competitive manner.
journal_name
Psychoneuroendocrinologyjournal_title
Psychoneuroendocrinologyauthors
Bengtsson SK,Nyberg S,Hedström H,Zingmark E,Jonsson B,Bäckström T,Bixo Mdoi
10.1016/j.psyneuen.2014.10.025subject
Has Abstractpub_date
2015-02-01 00:00:00pages
22-31eissn
0306-4530issn
1873-3360pii
S0306-4530(14)00409-0journal_volume
52pub_type
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journal_title:Psychoneuroendocrinology
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pub_type: 杂志文章,随机对照试验
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journal_title:Psychoneuroendocrinology
pub_type: 临床试验,杂志文章,随机对照试验
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pub_type: 杂志文章
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pub_type: 杂志文章,随机对照试验
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