Neurosteroids gaba a receptor function

In a comparative study on 189 patients with adjustment disorder with anxiety, one group of patients took 150mg of Stresam daily for 28 days, while the other group took 2mg of Lorazepam (Ativan). The treatment efficiency was similar for both drugs regarding mean HAM-A score. However, more people from etifoxine group responded to the treatment by the day 28 (72% and 56%). The first group also experienced fewer side effects compared to lorazepam group and fewer cases of rebound anxiety. Similar results were obtained in the comparative study of Stresam with Alprazolam (Xanax).

In the mid 1980s, the neuroactive steroids 3α,5α-tetrahydroprogesterone or allopregnanolone (3α,5α-THP) and 3α,5α- tetrahydrodeoxycorticosterone (3α,5α-THDOC) were shown to modulate neuronal excitability via their interaction with GABA A receptors. The steroids 3α,5α-THP and 3α,5α-THDOC were able to enhance the GABA-elicited Cl − current. [13] In addition, these steroids might enhance the binding of muscimol and benzodiazepines to GABA A receptors. [30] Structure- activity studies (SAR) showed that the 3alpha-OH group is essential for the anesthetic actions of these steroids, [31] they also have an optimally-placed hydrogen bond accepting group on the β face of the steroid at the C-17 position. The four steroid rings form a rigid framework for positioning these hydrogen groups in three-dimensional space. [32] Analogues 5 and 6 (Figure 10) are weak modulators of GABA A receptor function because the flexible side chains in these analogues do not have the conformations required for high biological activity. [33]

Benzodiazepines may influence neurosteroid metabolism by virtue of their actions on translocator protein (TSPO; "peripheral benzodiazepine receptor"). [59] The pharmacological actions of benzodiazepines at the GABA A receptor are similar to those of neurosteroids . Factors which affect the ability of individual benzodiazepines to alter neurosteroid levels may depend upon whether the individual benzodiazepine drug interacts with TSPO. Some benzodiazepines may also inhibit neurosteroidogenic enzymes reducing neurosteroid synthesis. [60]

In general, GABA does not cross the blood–brain barrier , [50] although certain areas of the brain that have no effective blood–brain barrier, such as the periventricular nucleus , can be reached by drugs such as systemically injected GABA. [57] At least one study suggests that orally administered GABA increases the amount of human growth hormone (HGH). [58] GABA directly injected to the brain has been reported to have both stimulatory and inhibitory effects on the production of growth hormone, depending on the physiology of the individual. [57] Certain pro-drugs of GABA (ex. picamilon ) have been developed to permeate the blood–brain barrier, then separate into GABA and the carrier molecule once inside the brain. This allows for a direct increase of GABA levels throughout all areas of the brain, in a manner following the distribution pattern of the pro-drug prior to metabolism. [ citation needed ]

Neurosteroids gaba a receptor function

neurosteroids gaba a receptor function

In general, GABA does not cross the blood–brain barrier , [50] although certain areas of the brain that have no effective blood–brain barrier, such as the periventricular nucleus , can be reached by drugs such as systemically injected GABA. [57] At least one study suggests that orally administered GABA increases the amount of human growth hormone (HGH). [58] GABA directly injected to the brain has been reported to have both stimulatory and inhibitory effects on the production of growth hormone, depending on the physiology of the individual. [57] Certain pro-drugs of GABA (ex. picamilon ) have been developed to permeate the blood–brain barrier, then separate into GABA and the carrier molecule once inside the brain. This allows for a direct increase of GABA levels throughout all areas of the brain, in a manner following the distribution pattern of the pro-drug prior to metabolism. [ citation needed ]

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