Cilobradine (hydrochloride)

Cilobradine hydrochloride is a HCN channel blocker. Cilobradine hydrochloride induces cardiac pacemaker currents and produces antidepressant effects[1][2][3][4][5].

Product Specifications

CAS Number

[186097-54-1]

Product Name Alternative

DK-AH 269

UNSPSC

12352005

Target

HCN Channel

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/Cilobradine-hydrochloride.html

Purity

99.73

Solubility

DMSO : ≥ 125 mg/mL|H2O : 100 mg/mL (ultrasonic)

Smiles

O=C1N(C[C@@H]2CN(CCC3=CC=C(OC)C(OC)=C3)CCC2)CCC4=CC(OC)=C(OC)C=C4C1.[H]Cl

Molecular Formula

C28H39ClN2O5

Molecular Weight

519.07

References & Citations

[1]Cheng L, et al. Molecular mapping of the binding site for a blocker of hyperpolarization-activated, cyclic nucleotide-modulated pacemaker channels. J Pharmacol Exp Ther. 2007 Sep;322 (3) :931-939.|[2]Van Bogaert PP, et al. Use-dependent blockade of cardiac pacemaker current (If) by cilobradine and zatebradine. Eur J Pharmacol. 2003 Oct 8;478 (2-3) :161-71.|[3]Stieber J, et al. Bradycardic and proarrhythmic properties of sinus node inhibitors. Mol Pharmacol. 2006 Apr;69 (4) :1328-37.|[4]Umeya N, et al. Detection of retinal dysfunction induced by HCN channel inhibitors using multistep light stimulus and long-duration light stimulus ERG in rats. Exp Eye Res. 2024 Apr;241:109847. |[5]Cai M, et al. HCN channel inhibitor induces ketamine-like rapid and sustained antidepressant effects in chronic social defeat stress model. Neurobiol Stress. 2023 Aug 19;26:100565.