Neurosteroid modulation of synaptic and extrasynaptic gabaa receptors

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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]

Our focus is selective modulation of neuronal ion channels, which are among the most critical CNS targets. Our lead candidates, NCT-10004 and NCT-10001, effectively relieve itch and pain in animal models. Our neurosteroid program focuses on effective treatment of refractory epilepsy and postpartum depression. Our unique biocatalytic medicinal chemistry platform allows us to make drug structures that our competitors can’t. This allows us to realize the full potential of the privileged drug scaffolds that have served as the foundation for numerous important therapeutics.

Neurosteroid modulation of synaptic and extrasynaptic gabaa receptors

neurosteroid modulation of synaptic and extrasynaptic gabaa receptors

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neurosteroid modulation of synaptic and extrasynaptic gabaa receptorsneurosteroid modulation of synaptic and extrasynaptic gabaa receptorsneurosteroid modulation of synaptic and extrasynaptic gabaa receptorsneurosteroid modulation of synaptic and extrasynaptic gabaa receptorsneurosteroid modulation of synaptic and extrasynaptic gabaa receptors

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