2. GPCR/G Protein Neuronal Signaling Membrane Transporter/Ion Channel
  3. Adrenergic Receptor Sodium Channel Potassium Channel
  4. 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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ICI 147798

ICI 147798 Chemical Structure

CAS No. : 83812-65-1

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ICI 147798 Related Antibodies

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Description

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[1][2][3].

IC50 & Target[1]

β-adrenoceptor

8.8 (pkB)

In Vitro

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 Related Antibodies
In Vivo

ICI 147798 (0.125-0.75%; eye drop; single dose) produces statistically significant, concentration-dependent intraocular pressure (IOP)-lowering effects in unanesthetized New Zealand rabbits in a water load-induced high IOP model, with an ED50 of 0.27% for IOP reduction and a duration of action of 5 hours at the 0.5% dose[2].
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.

Animal Model: New Zealand rabbits (adult, 2-5 kg, both sexes, water-load-induced ocular hypertension model)[2]
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%
Administration: eye drop; single dose
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.
Molecular Weight

515.99

Formula

C24H30ClN7O4
CAS No.
SMILES

O=C(C1=NC(Cl)=C(N)N=C1N)NC(C)(C)C(NCCNCC(COC2=CC=CC3=C2C=CC=C3)O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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ICI 147798 Related Classifications

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Keywords:

ICI 14779883812-65-1ICI147798ICI-147798Adrenergic ReceptorSodium ChannelPotassium ChannelBeta ReceptorNa channelsNa+ channelsKcsAglaucomaadenylate cyclaseβ-adrenoceptorβ-1 adrenoceptorsNew Zealand rabbitstoad bladderguinea pig right atriaguinea pig tracheaβ-2 adrenoceptorshistamine H2-receptorInhibitorinhibitorinhibit

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