ZD7288 is a potent HCN blocker of hyperpolarization-activated cyclic nucleotide-gated channels (HCN channels) in heart and brain tissue. Recently shown to also block Na+ currents in DRG neurons and in HEK293 cells transfected with Na(v)1.4 plasmids. In voltage clamp experiments, it is shown to reduce Ih in a time- and concentration-dependent manner (IC50 = 2 mM). Suggested to behave as a lipophilic quaternary cation that can pass into the cell interior to block Ih channels in their closed state.
Acciones bioquímicas o fisiológicas
Primary Target HCN channel
Advertencia
Toxicity: Standard Handling (A)
Reconstitución
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Otras notas
Pleasenote that the molecular weight for this compound is batch-specific due tovariable water content.
Información legal
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Código de clase de almacenamiento
11 - Combustible Solids
Clase de riesgo para el agua (WGK)
WGK 3
Punto de inflamabilidad (°F)
Not applicable
Punto de inflamabilidad (°C)
Not applicable
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ZD7288 has been widely used as a tool in the study of hyperpolarization-activated cyclic nucleotide-gated channels (HCN channels), and to test the relationships between HCN channels and heart and brain function. ZD7288 is widely considered a selective blocker of HCN
Journal of neurophysiology, 74(6), 2366-2378 (1995-12-01)
1. The effects of the novel bradycardic agent 4-(N-ethyl-N-phenylamino)-1,2-dimethyl-6-(methylamino) pyrimidinium chloride (ZD 7288) (Zeneca) were investigated on the hyperpolarization-activated cationic current (Ih) in guinea pig substantia nigra pars compacta neurons in vitro, using a single-microelectrode current-clamp/voltage-clamp technique. 2. Under current-clamp
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