Cilobradine (hydrochloride)


CAS No. : 186097-54-1

(Synonyms: DK-AH 269)

186097-54-1
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Cat. No. : HY-18940A
M.Wt: 519.07
Formula: C28H39ClN2O5
Purity: >98 %
Solubility: H2O : 100 mg/mL (ultrasonic);DMSO : ≥ 125 mg/mL
Introduction of 186097-54-1 :

Cilobradine hydrochloride is a HCN channel blocker. Cilobradine hydrochloride induces cardiac pacemaker currents and produces antidepressant effects[1][2][3][4][5]. In Vitro:Cilobradine (1 μM) hydrochloride induces a use-dependent blockade of cardiac pacemaker current in rabbit sino-atrial cells[2].
Cilobradine blocks HCN channel currents in HEK293 cells expressing human HCN1, HCN2, HCN3, and HCN4 channels in a dose- and treatment-dependent manner, and its steady-state inhibition of different HCN isoforms is not isoform-specific[3].
In Vivo:Cilobradine (4-40 mg/kg; s.c,; single dose) hydrochloride can prolong the latency of the a-wave or b-wave of the rat electroretinogram (ERG), and a dose-dependent waveform change after the b-wave occurs at a specific light stimulus brightness[4].
. Cilobradine (intracerebroventricular injection dose 0.6 μg; intraperitoneal injection dose 20 mg/kg; intracerebroventricular microinjection and i.p.; single dose) hydrochloride can reverse depressive-like behavior, and the effect lasts for about two weeks[5].

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