| Hazard Information | Back Directory | [Description]
hCAI/II-IN-6 is an orally active human carbonic anhydrase (CA) inhibitor. hCAI/II-IN-6 selectively inhibits hCA II and hCA VII isoforms with Ki values of 220, 4.9, 6.5 and ??50000 nM for hCA I, hCA II , hCA VII and hCA XII respectively. hCAI/II-IN-6 shows anticonvulsant activity and anti maximal electroshock (MES) activity in vivo. hCAI/II-IN-6 can be used for the research of epilepsy[1]. hCAI/II-IN-6 (0-50 μM) inhibits hCA I, hCA II , hCA VII and hCA XII activities with Ki values of 220, 4.9, 6.5 and ??50000 nM, respectively[1]. hCAI/II-IN-6 (30-100mg/kg; i.p. once) shows good anticonvulsant effect in vivo[1].
hCAI/II-IN-6 (30 mg/kg; p.o. once) shows anti-MES activity in vivo[1]. | [Uses]
hCAI/II-IN-6 is an orally active human carbonic anhydrase (CA) inhibitor. hCAI/II-IN-6 selectively inhibits hCA II and hCA VII isoforms with Ki values of 220, 4.9, 6.5 and ＞50000 nM for hCA I, hCA II , hCA VII and hCA XII respectively. hCAI/II-IN-6 shows anticonvulsant activity and anti maximal electroshock (MES) activity in vivo. hCAI/II-IN-6 can be used for the research of epilepsy[1]. | [in vivo]
hCAI/II-IN-6 (30-100mg/kg; i.p. once) shows good anticonvulsant effect in vivo[1].
hCAI/II-IN-6 (30 mg/kg; p.o. once) shows anti-MES activity in vivo[1]. | Animal Model: | Swiss albino mice[1] | | Dosage: | 30 and 100 mg/kg | | Administration: | Intraperitoneal injection; 30-100 mg/kg once | | Result: | Provided seizure attenuation and good anticonvulsant effect, and showed an ED50 of 13.7mg/kg in anticonvulsant quantification study.
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| Animal Model: | Wistar albino rats[1] | | Dosage: | 30 mg/kg | | Administration: | Oral gavage; 30 mg/kg once | | Result: | Showed anti-MES activity and significant protection from seizures up to 1h of drug administration and action was gone reduced after 1h. |
| [References]
[1] Mishra CB, et al. Discovery of Benzenesulfonamides with Potent Human Carbonic Anhydrase Inhibitory and Effective Anticonvulsant Action: Design, Synthesis, and Pharmacological Assessment. J Med Chem. 2017 Mar 23;60(6):2456-2469. DOI:10.1021/acs.jmedchem.6b01804 |
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