Name | ICI-118551 HCL |
Synonyms | ICI-118551 ICI-118551 HCL 3-(isopropylamino)-1-((7-methyl-2,3-dihydro-1H-inden-4-yl)oxy)butan-2-ol hydrochloride |
CAS | 1217094-53-5 |
Molecular Formula | C17H28ClNO2 |
Molar Mass | 313.87 |
Storage Condition | -20℃ |
In vitro study | ICI-118551 inhibit the accumulation of cAMP, IC50 = 1.7 mM. In isolated perfused lung models, ICI-118551 treatment increased pulmonary lumen diameter and decreased pulmonary artery pressure under both normoxic and hypoxic conditions. Transgenic mice (high expression of β2 adrenoceptors, high G (I) levels) had a similar negative inotropic response after treatment with ICI 118,551, although they had normal basal contractions. Over-expression of human β2 adrenoceptors in rabbit-derived myocytes potentiates the negative inotropic effects of ICI 118,551. In human, rabbit, and mouse myocytes, treatment with pertussis toxin inactivated G (I) inhibited this negative inotropic effect, and overexpression of Giα2 reinduced the modified effect in normal rabbit-derived myocytes. |
In vivo study | ICI 118,551 had no effect on β1 receptor-mediated shortening of electromechanical contractility, elevation of systolic blood pressure, and upregulation of renin. Like propiolol, a drug used to treat arrhythmias, angina, etc., it inhibits the β2 receptor-mediated lowering of diastolic blood pressure and the upregulation of norepinephrine. After inhibition of β2 receptors by ICI 118,551, blood pressure was lowered. |