Description
ICA-110381 (325457-99-6) is a KCNQ2/Q3 (Kv7.2/7.3) activator, EC50=0.38 μM (KCNQ1 IC50=15 μM).1KCNQ3/Q5 heterodimers are not affected2. Potently dampens neuronal excitability and displays anticonvulsant activityin vivo.2
Uses
ICA 110381 was used to study the pharmacological activities as it selectively activated human KCNQ2 expressed in Chinese hamster ovary, damped neuronal excitability in rat hippocampal CA1 cell and showed anticonvulsant activity in amygdala-kindled rat.
in vivo
ICA 110381 (3-30 mg/kg; p.o.; once) elevates the threshold for induction of afterdischarges and reduced seizure severity and duration in fully amygdala-kindled rats[2].
| Animal Model: | Female Wistar rats (200-300 g)[2] |
| Dosage: | 3 mg/kg, 10 mg/kg and 30 mg/kg (suspended in 0.5% Hydroxyethyl Cellulose (HY-B2221B)) |
| Administration: | Oral administration; once |
| Result: | Showed anticonvulsive properties in fully amygdala-kindled rats. |
IC 50
KV7.1: 0.38 μM (EC
50); KV7.3: 0.38 μM (EC
50); KV7.1: 15 μM (IC
50)
References
[1] GEORGE AMATO. N-Pyridyl and Pyrimidine Benzamides as KCNQ2/Q3 Potassium Channel Openers for the Treatment of Epilepsy[J]. ACS Medicinal Chemistry Letters, 2011, 2 6: 481-484. DOI:
10.1021/ml200053x[2] A BOEHLEN. The new KCNQ2 activator 4-Chlor-N-(6-chlor-pyridin-3-yl)-benzamid displays anticonvulsant potential[J]. British Journal of Pharmacology, 2012, 168 5: 1182-1200. DOI:
10.1111/bph.12065
