2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. Histamine Receptor
  4. 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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SCH 79687

SCH 79687 Chemical Structure

CAS No. : 224585-45-9

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SCH 79687 Related Antibodies

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Description

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[1].

In Vitro

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 Related Antibodies
Parmacokinetics
Species Dose Route AUC T1/2 Cmax Tmax
Rat[1] 10 mg/kg p.o. 18.1 μg·h/mL / 1.5 μg/mL 4.5 h
Monkey[1] 3 mg/kg p.o. 12.6 μg·h/mL / 1.7 μg/mL 4.4 h
Monkey[1] 3 mg/kg i.v. 24.1 μg·h/mL 2.5 h / /
In Vivo

SCH 79687 (0.03-3 mg/kg; intravenous injection; single administration) dose-dependently attenuates the inhibitory effect of (R)-α-methylhistamine on sympathetic hypertensive responses in guinea pigs, with an intravenous ED50 of 0.28 mg/kg[1].
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.

Animal Model: Hartley (male, anesthetized)[1]
Dosage: 0.03 mg/kg; 0.3 mg/kg; 3.0 mg/kg
Administration: i.v.; single dose; 5 min prior to (R)-α-methylhistamine
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.).
Animal Model: (anesthetized)[1]
Dosage: 3 mg/kg (i.v., combined with loratadine); 10 mg/kg (p.o., combined with loratadine)
Administration: i.v.; single dose; 30 min prior to compound 48/80; p.o.; single dose; 2 h prior to compound 48/80
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.
Molecular Weight

375.25

Formula

C18H16Cl2N4O
CAS No.
SMILES

O=C(NCC1=CC=C(CC2=CN=CN2)C=C1)NC3=CC(Cl)=CC(Cl)=C3
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Storage

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Purity & Documentation
References
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SCH 79687 Related Classifications

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Keywords:

SCH 79687224585-45-9SCH79687SCH-79687Histamine Receptorratimidazoline I2 receptors(R)-α-methylhistaminehistamine H3 receptorα2A-adrenoceptorsallergic rhinitisguinea pighistamine H3 receptorshistamine H1 receptorscatsInhibitorinhibitorinhibit

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