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

SCH 79687 是一种具有口服活性的组胺 H3 受体 (histamine H3 receptor) 拮抗剂，其大鼠 Ki 为 1.9 nM，豚鼠 Ki 为 13 nM。SCH 79687 可作为竞争性拮抗剂发挥作用以对抗 (R)-α-甲基组胺。SCH 79687 可减弱豚鼠体内由 (R)-α-甲基组胺诱导的交感神经高血压反应抑制作用。SCH 79687 与 H1 拮抗剂联合使用时，可抑制猫体内由 Compound 48/80 (HY-115768) 诱导的鼻充血。SCH 79687 可用于过敏性鼻炎的研究。

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SCH 79687

SCH 79687 Chemical Structure

CAS No. : 224585-45-9

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SCH 79687 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

SCH 79687 (1.9-13 nM; 30 min) 可高亲和力结合大鼠和豚鼠组胺 H3 受体 (Ki = 1.9 nM 和 13 nM)，对 H1、H2、α2A-肾上腺素能受体以及咪唑啉 I2 受体的结合能力极弱[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

SCH 79687 相关抗体:
药代动力学
(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 / /
体内研究
(In Vivo)

SCH 79687 (0.03-3 mg/kg; 静脉注射；单次) 可剂量依赖性地减弱 (R)-α-甲基组胺对豚鼠交感神经高血压反应的抑制作用，其静脉注射 ED50 为 0.28 mg/kg[1]。
SCH 79687 (3-10 mg/kg；静脉注射、口服；单剂量) 与 Loratadine (HY-17043) 联合使用时，在猫 Compound 48/80 诱导的鼻充血模型中，通过静脉注射 (3 mg/kg) 和口服 (10 mg/kg) 两种途径均能产生显著的减充血疗效，且不会升高血压[1]。

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.
分子量

375.25

Formula

C18H16Cl2N4O
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

SCH 79687 相关分类

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  • Do most proteins show cross-species activity?

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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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