Home GPCR & G Protein Adrenergic Receptor antagonist Zenidolol (ICI-118551) Hydrochloride For research use only.

Zenidolol (ICI-118551) Hydrochloride

Synonyms: ICI-118,551

Zenidolol (ICI-118551) Hydrochloride is a highly selective β2-adrenergic receptor antagonist with Ki values of 0.7, 49.5 and 611 nM for β2, β1 and β3 receptors, respectively.

Zenidolol (ICI-118551) Hydrochloride Chemical Structure

Zenidolol (ICI-118551) Hydrochloride Chemical Structure

CAS No. 72795-01-8

Purity & Quality Control

Zenidolol (ICI-118551) Hydrochloride Related Products

Signaling Pathway

Adrenergic Receptor Signaling Pathways

Adrenergic Receptor Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CHO Function assay 120 mins Displacement of [3H]CGP 12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells measured after 120 mins by scintillation counting method, IC50=0.00074μM 27876250
CHOK1 Function assay 2 hrs Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method, Kd=0.0002455μM 28523097
CHOK1 Function assay 2 hrs Displacement of [3H](-)CGP12177 from human beta1-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method, Kd=0.18197μM 28523097
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Biological Activity

Description Zenidolol (ICI-118551) Hydrochloride is a highly selective β2-adrenergic receptor antagonist with Ki values of 0.7, 49.5 and 611 nM for β2, β1 and β3 receptors, respectively.
Targets
β2-adrenergic receptor [1]
(Cell-free assay)		 β1-adrenergic receptor [1]
(Cell-free assay)		 β3-adrenoceptor [1]
(Cell-free assay)
0.7nM(Ki) 49.5nM(Ki) 611nM(Ki)
In vitro
In vitro

ICI-118551 inhibits cAMP accumulation by 50% (IC50 = 1.7 mM)[1].  ICI 118551 increases vascular lumen diameter in lung sections and reduces pulmonary arterial pressure under normoxia and under hypoxia in the isolated perfused lung model[2]. Transgenic mice with high beta(2)AR number and increased G(i) levels have normal basal contractility but show a similar negative inotropic response to ICI 118,551. Overexpression of human beta(2)AR in rabbit myocytes using adenovirus potentiates the negative inotropic effect of ICI 118,551. In human, rabbit, and mouse myocytes, the negative inotropic effects are blocked after treatment of cells with pertussis toxin to inactivate G(i), and overexpression of G(i)alpha(2) induces the effect de novo in normal rat myocytes[5].
Cell Research Cell lines MEF cell line
Concentrations 10μM
Incubation Time 2-hours incubation at room-temperature
Method

Binding reactions are carried out by incubating 60 μg of membranes with 10 nM [3H]dihydroalprenolol hydrochloride and different concentrations of ICI 118,551. After a two hour incubation at room-temperature, the binding reactions are terminated by rapid filtration over glass fiber filters. Radioactivity in the filters is then quantified using a liquid scintillation counter. Non-specific binding is determined in the presence of 1 μM alprenolol. Binding data are analyzed with GraphPad Prism software.
In Vivo
In vivo

After 1 week of treatment, ICI 118,551 has no effect on the beta 1-receptor mediated shortening of electromechanical systole (QS2I), the rise in systolic pressure and rise in renin, whereas these responses are blocked by a dose factor of eight. ICI 118,551 and equally block the beta 2-receptor mediated fall in diastolic pressure and the rise in noradrenaline. beta 2-selective blockade by ICI 118,551 lowers blood pressure[4].
Animal Research Animal Models 8-9 weeks old male mice
Dosages 1 or 2 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 313.86 Formula

C17H27NO2.HCl
CAS No. 72795-01-8 SDF Download Zenidolol (ICI-118551) Hydrochloride SDF
Smiles CC1=C2CCCC2=C(C=C1)OCC(C(C)NC(C)C)O.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 62 mg/mL ( (197.54 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 62 mg/mL

Water : 21 mg/mL


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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