KMCA-0011 is an orally active ɑ 2C adrenoceptor antagonist ( K i = 56.7 nM). KMCA-0011 alleviates depressive behaviors by enhancing BDNF and synaptic plasticity. KMCA-0011 displays favorable metabolic stability, including high plasma stability (99.8% after 120 min). KMCA-0011 can be used for the research of depression [1].
In Vivo, KMCA-0011 (Compound 11e) (1-10 mg/kg, p.o., daily for one week) shows the most consistent behavioral efficacy across multiple tests, uniquely ameliorates anxiety-like behavior in the EPM test, increases hippocampal BDNF expression and restores CORT-induced impairments in synaptic plasticity in the Maternal separation (MS) mouse model[1].
In Vitro, KMCA-0011 (Compound 11e) exhibits notably high binding affinity toward ɑ2C Adrenoceptor (Ki = 56.7 nM) in human HEK-293 cells[1]. KMCA-0011 (10 μM) effectively inhibits Epinephrine-induced ERK phosphorylation[1].
References:
[1]. Seo K, et al. ɑ2C Adrenoceptor antagonist KMCA-0011 alleviated depressive-like behaviors in a maternal separation mouse model. Bioorg Med Chem Lett. 2026 Feb 1;131:130467.
In Vivo, KMCA-0011 (Compound 11e) (1-10 mg/kg, p.o., daily for one week) shows the most consistent behavioral efficacy across multiple tests, uniquely ameliorates anxiety-like behavior in the EPM test, increases hippocampal BDNF expression and restores CORT-induced impairments in synaptic plasticity in the Maternal separation (MS) mouse model[1].
In Vitro, KMCA-0011 (Compound 11e) exhibits notably high binding affinity toward ɑ2C Adrenoceptor (Ki = 56.7 nM) in human HEK-293 cells[1]. KMCA-0011 (10 μM) effectively inhibits Epinephrine-induced ERK phosphorylation[1].
References:
[1]. Seo K, et al. ɑ2C Adrenoceptor antagonist KMCA-0011 alleviated depressive-like behaviors in a maternal separation mouse model. Bioorg Med Chem Lett. 2026 Feb 1;131:130467.