Figures & data
Figure 1. Structures of histamine H3 receptor ligands with anticonvulsant activity, triazole derivatives with anticonvulsant activity and target compounds 3a-3q designed.
![Figure 1. Structures of histamine H3 receptor ligands with anticonvulsant activity, triazole derivatives with anticonvulsant activity and target compounds 3a-3q designed.](/cms/asset/ef2ab693-edca-48de-875d-f315283ccc3e/ienz_a_1774573_f0001_c.jpg)
Table 1. H3R antagonistic activity of compounds 3a-3q.
Figure 2. Effects of compounds 3a, 3c, 3h, 3k, 3l, and 3m on the level of intracellular cAMP administrated alone.
![Figure 2. Effects of compounds 3a, 3c, 3h, 3k, 3l, and 3m on the level of intracellular cAMP administrated alone.](/cms/asset/32bcb708-debe-41a6-8768-0a792518fc83/ienz_a_1774573_f0002_c.jpg)
Figure 4. The predicted configurations for PIT (A), 3h (B) and 3m (C) binding with H3R, and their overlying pattern (D).
![Figure 4. The predicted configurations for PIT (A), 3h (B) and 3m (C) binding with H3R, and their overlying pattern (D).](/cms/asset/7350ba2a-f35b-4f3c-88bc-b2752f44c6b0/ienz_a_1774573_f0004_c.jpg)
Figure 5. Effects of H3R antagonists/inverse agonists 3a-3q (10 mg/kg, i.p.), PIT (10 mg/kg, i.p.) and anticonvulsant drug VPA (300 mg/kg, i.p.) against MES-induced convulsions. Protection for mice was defined as the reduction or abolition of the tonic hind limb extension (THLE) in MES model. Results are showed as mean ± SEM with seven animals in each group. Values are considered significant at *p < 0.05, **p < 0.01, ***p < 0.001, ****p < 0.0001 as compared to saline-treated group.
![Figure 5. Effects of H3R antagonists/inverse agonists 3a-3q (10 mg/kg, i.p.), PIT (10 mg/kg, i.p.) and anticonvulsant drug VPA (300 mg/kg, i.p.) against MES-induced convulsions. Protection for mice was defined as the reduction or abolition of the tonic hind limb extension (THLE) in MES model. Results are showed as mean ± SEM with seven animals in each group. Values are considered significant at *p < 0.05, **p < 0.01, ***p < 0.001, ****p < 0.0001 as compared to saline-treated group.](/cms/asset/de5efd06-bc28-4f72-9068-5e9b7efbeed3/ienz_a_1774573_f0005_b.jpg)
Figure 6. Effects of compounds 3a-3q (10 mg/kg, i.p.), and reference drug PIT (10 mg/kg, i.p.) and VPA (300 mg/kg, i.p.) against PTZ-induced convulsions. Results are showed as mean ± SEM of seven mice in each group. & represent full protection.
![Figure 6. Effects of compounds 3a-3q (10 mg/kg, i.p.), and reference drug PIT (10 mg/kg, i.p.) and VPA (300 mg/kg, i.p.) against PTZ-induced convulsions. Results are showed as mean ± SEM of seven mice in each group. & represent full protection.](/cms/asset/689254c1-3726-45d0-9f65-0c7f52cc8750/ienz_a_1774573_f0006_b.jpg)
Figure 7. Protective effects of compound 3m and reference drug PIT against MES-induced convulsions in different doses. Protection in the test was defined as the reduction or abolition of the THLE in mice. Results were showed as mean ± SEM with seven animals in each group. Values are considered significant at *p < 0.05, **p < 0.01, ***p < 0.001 when compared to saline-treated group. &PIT, at 20 mg/kg dose, fully abrogate the THLE for all the tested mice.
![Figure 7. Protective effects of compound 3m and reference drug PIT against MES-induced convulsions in different doses. Protection in the test was defined as the reduction or abolition of the THLE in mice. Results were showed as mean ± SEM with seven animals in each group. Values are considered significant at *p < 0.05, **p < 0.01, ***p < 0.001 when compared to saline-treated group. &PIT, at 20 mg/kg dose, fully abrogate the THLE for all the tested mice.](/cms/asset/6bd0e2ed-f75a-45b2-b725-31acfc006149/ienz_a_1774573_f0007_b.jpg)
Figure 8. Protective effects of compound 3m (10 mg/kg, i.p.) against MES-induced convulsions when pre-treatment of RAMH (10 mg/kg, i.p.). Protection in the test was defined as the reduction or abolition of the THLE in mice. Results are showed as mean ± SEM with seven animals in each group. Values are considered significant at *p < 0.01 as compared to saline-treated group, and #p < 0.01 as compared to 3m + RAMH treated group.
![Figure 8. Protective effects of compound 3m (10 mg/kg, i.p.) against MES-induced convulsions when pre-treatment of RAMH (10 mg/kg, i.p.). Protection in the test was defined as the reduction or abolition of the THLE in mice. Results are showed as mean ± SEM with seven animals in each group. Values are considered significant at *p < 0.01 as compared to saline-treated group, and #p < 0.01 as compared to 3m + RAMH treated group.](/cms/asset/f6e6f0d4-f0a7-44e2-be49-dae124b6bb5e/ienz_a_1774573_f0008_b.jpg)