Table 3.
Binding Affinities, Pharmacological Properties and Proposed Biding Sites of LTG and Similar Compounds [54]
KD [µM] Rat Brain Na+ Channels (NaV1.2) Expressed in Xenopus oocytes in Inactivated State (- 50 mV) | Pharmacological Properties in Preclinical Evaluation | Position of Amino Acid Residues in IV- S6 Binding Site | |
---|---|---|---|
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17.3 | Analgesic but no anticonvulsant activity | 1764 – strong interaction |
1771 – strong interaction | |||
1760 – weaker interaction | |||
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3.7 | Analgesic and anticonvulsant activity | 1764 – much stronger interaction; |
1771 – modest interaction; | |||
1760 weaker interaction | |||
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10.3 | Prevention of neuronal toxicity following stroke | 1764 – strong interaction; |
1771 – weak interaction; | |||
1760 – weak interaction; | |||
Possible interactions with amino acid | |||
Residues in other transmembrane segments |