SCH 79687
SCH 79687 is an orally active histamine H3 receptor antagonist, with a Ki of 1.9 nM in rats and 13 nM in guinea pigs. SCH 79687 acts as a competitive antagonist against (R)-α-methylhistamine. SCH 79687 attenuates the inhibitory effect of (R)-α-methylhistamine-induced sympathetic hypertensive responses in guinea pigs. When used in combination with H1 antagonists, SCH 79687 inhibits Compound 48/80 (HY-115768)-induced nasal congestion in cats. SCH 79687 can be used for the research of allergic rhinitis.
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- CAS No.: 224585-45-9
- Formule: C18H16Cl2N4O
- Masse moléculaire:375.25
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
SCH 79687 (1.9-13 nM; 30 min) binds to rat and guinea pig histamine H3 receptors with high affinity (Ki = 1.9 nM and 13 nM), and exhibits extremely weak binding affinity to H1, H2, α2A-adrenergic receptors and imidazoline I2 receptors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
SCH 79687 (3-10 mg/kg; intravenous injection, oral administration; single dose) exerts significant decongestant effects via both intravenous (3 mg/kg) and oral (10 mg/kg) routes in a feline model of nasal congestion induced by Compound 48/80 (HY-115768), without increasing blood pressure, when used in combination with Loratadine (HY-17043)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Hartley (male, anesthetized)[1]
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Dosage:0.03 mg/kg; 0.3 mg/kg; 3.0 mg/kg
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Administration:i.v.; single dose; 5 min prior to (R)-α-methylhistamine
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Result:Produced a dose-dependent attenuation of (R)-α-methylhistamine-induced inhibition of sympathetic hypertensive responses, with an ED50 of 0.28 mg/kg i.v.
Inhibited the (R)-α-methylhistamine response by ~10% at 0.03 mg/kg i.v.
Inhibited the (R)-α-methylhistamine response by ~65% at 0.3 mg/kg i.v.
Inhibited the (R)-α-methylhistamine response by ~80% at 3.0 mg/kg i.v.
Reached a mean plasma concentration of 25 ng/mL at 30 min post-dose at the ED50 dose (0.28 mg/kg i.v.).
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Animal Model:(anesthetized)[1]
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Dosage:3 mg/kg (i.v., combined with loratadine); 10 mg/kg (p.o., combined with loratadine)
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Administration:i.v.; single dose; 30 min prior to compound 48/80; p.o.; single dose; 2 h prior to compound 48/80
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Result:Significantly blocked compound 48/80-induced increases in nasal resistance when administered intravenously at 3 mg/kg in combination with loratadine (3 mg/kg i.v.), with no effect on mean arterial blood pressure.
Significantly inhibited compound 48/80-induced decreases in nasal cavity volume when administered orally at 10 mg/kg in combination with loratadine (10 mg/kg p.o.), with no effect on systolic blood pressure.
Did not alter nasal responses to compound 48/80 when administered alone at either dose.
Chemical Information
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CAS No. 224585-45-9
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Masse moléculaire 375.25
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Formule C18H16Cl2N4O
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SMILES
O=C(NCC1=CC=C(CC2=CN=CN2)C=C1)NC3=CC(Cl)=CC(Cl)=C3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SCH 79687 Related Classifications
HY-182296 Related Classifications
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