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. 2013 Apr;20(10):1241–1285. doi: 10.2174/0929867311320100005

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

graphic file with name CMC-20-1241_T3S1.jpg 17.3 Analgesic but no anticonvulsant activity 1764 – strong interaction
1771 – strong interaction
1760 – weaker interaction

graphic file with name CMC-20-1241_T3S2.jpg 3.7 Analgesic and anticonvulsant activity 1764 – much stronger interaction;
1771 – modest interaction;
1760 weaker interaction

graphic file with name CMC-20-1241_T3S3.jpg 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