ICI 147798
ICI 147798 is an orally effective β-adrenoceptor antagonist with a pKB of 9.1 (in guinea pig right atrium) and 8.8 (in guinea pig trachea). ICI 147798 acts as a diuretic and intraocular pressure-lowering agent. ICI 147798 blocks β-adrenoceptors, inhibits isoproterenol-induced tachycardia and vasodepressor responses, exhibits slowly dissociating, insurmountable antagonism against β1-adrenoceptors, and shows surmountable competitive antagonism against β2-adrenoceptors. ICI 147798 induces natriuresis and kaliuresis, inhibits sodium transport, and reduces intraocular pressure.
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- No. CAS: 83812-65-1
- Fòrmula: C24H30ClN7O4
- Peso molecular:515.99
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Chemical Information
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Actividad biológica
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β-adrenoceptor 8.8 (pkB) |
ICI 147798 inhibits Na+ transport in isolated toad bladder preparations with mucosal and serosal IC50 values of 56 μM and 120 μM, respectively[1].
ICI 147798 acts as a beta-adrenoceptor antagonist in isolated guinea pig right atria with a pKB value of 9.1[1].
ICI 147798 acts as a beta-adrenoceptor antagonist in isolated guinea pig trachea with a pKB value of 8.8[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
ICI 147798 (0.1-1.0 mg/kg; intravenous administration) acts as a potent intravenous β-adrenergic receptor antagonist in unanesthetized New Zealand rabbits, with an ED50 of 0.23 mg/kg for blocking isoproterenol-induced tachycardia[2].
ICI 147798 (0.5%; topical administration; single dose, twice daily for 4 consecutive days) exerts no significant blocking effect on isoproterenol-induced tachycardia in unanesthetized New Zealand rabbits, even after twice-daily administration for 4 consecutive days[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:New Zealand rabbits (adult, 2-5 kg, both sexes, water-load-induced ocular hypertension model)[2]
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Dosage:300 μl, 0.5%; 200 μl, 0.5%; 200 μl, 0.125%; 200 μl, 0.25%; 100 μl, 0.5%; 200 μl, 0.75%; 100 μl, 0.75%
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Administration:eye drop; single dose
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Result:Reduced mean water-load-induced IOP increase to 4.0 mmHg at 1 hour, 5.3 mmHg at 3 hours, and 6.2 mmHg at 5 hours after 300 μl, 0.5% topical dosing to one eye.
Reduced mean water-load-induced IOP increase to 4.5 mmHg (left eye) and 4.0 mmHg (right eye) at 1 hour after 200 μl, 0.5% topical dosing to both eyes (P<0.05 vs control).
Exhibited concentration-dependent IOP-lowering effect with an ED50 of 0.27%.
Reduced mean water-load-induced IOP increase to 5.5 mmHg (left eye) and 5.5 mmHg (right eye) after 100 μl, 0.5% dosing in 5% PEG 400 + 5% Pluronic F127 vehicle.
Showed no enhanced IOP-lowering efficacy with 0.75% concentration or 200 μl volume, with mean ΔmmHg values ranging from 5.0 to 5.5 mmHg.
Chemical Information
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No. CAS 83812-65-1
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Peso molecular 515.99
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Fòrmula C24H30ClN7O4
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SMILES
O=C(C1=NC(Cl)=C(N)N=C1N)NC(C)(C)C(NCCNCC(COC2=CC=CC3=C2C=CC=C3)O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Kau ST, et al. ICI 147,798: a novel diuretic agent with beta adrenoceptor blocking activity. J Pharmacol Exp Ther. 1987;242(3):818-826. [Content Brief]
[2]. Kau ST, et al. On the topically effective ocular hypotensive properties of ICI 147,798, a natriuretic beta-adrenoceptor antagonist, in rabbits. Pharmacol Toxicol. 1989;64(1):132-136. [Content Brief]
[3]. Keith RA, et al. ICI 147,798: a slowly dissociable beta adrenoceptor antagonist that causes insurmountable beta-1 and surmountable beta-2 adrenoceptor antagonism in isolated tissues. J Pharmacol Exp Ther. 1989;248(1):240-248. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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