1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. Frovatriptan succinate

Frovatriptan succinate (Synonyms: (R)-Frovatriptan succinate; SB 209509 succinate; VML 251 succinate)

目录号: HY-B1658B
产品使用指南

Frovatriptan succinate ((R)-Frovatriptan succinate) 是一种强效,高亲和力,选择性和具有口服活性的 5-HT1B (pK50 为 8.2) 和 5-HT1D 受体激动剂,选择性是 5-HT1A,5-HT1F 和 5-HT7 的 10 倍以上,是其他 5-HT,多巴胺,组胺 H1 和 α1-肾上腺素受体的 1000 倍以上。Frovatriptan succinate 可用于偏头痛的研究。

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Frovatriptan succinate Chemical Structure

Frovatriptan succinate Chemical Structure

CAS No. : 158930-09-7

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Description

Frovatriptan succinate ((R)-Frovatriptan succinate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate has the potential for migraine research[1][2].

IC50 & Target[2]

5-HT1B Receptor

8.2 (pEC50)

5-HT1D Receptor

 

In Vitro

Cerebral vasodilatation and neurogenic inflammation are considered to be prime movers in the pathogenesis of migraine. Activation of 5-HT1B reverses cerebral vasodilatation and activation of 5-HT1D prevents neurogenic inflammation. Frovatriptan has a high affinity for 5-HT1B and 5-HT1D receptors and a moderate affinity for the 5-HT1A and 5-HT1F receptors subtypes. Frovatriptan has a moderate affinity for the 5-HT7 receptors, an action associated with coronary artery relaxation in the dog[1].

In Vivo

Oral bioavailability of Frovatriptan is 22%-30% and is not affected by food. Although the maximum concentration in the plasma is achieved in 2-3 hours, 60%-70% of this is achieved in 1 hour. A steady state is achieved in 4-5 days. Plasma protein binding is low at 15%. The most unique feature is the relative terminal long half-life of about 26 hours. Frovatriptan is chiefly metabolized by CYP1A2 and is cleared by the kidney and liver making moderate failure of either organ not a limiting factor in treatment[1].
Frovatriptan (0.1, 0.2, and 0.3 mg/kg; a single bolus intraduodenal administration) treatment produces an increase in carotid vascular resistance, which is sustained for at least 5 hours in dogs[2].

Molecular Weight

361.39

Formula

C₁₈H₂₃N₃O₅

CAS No.

158930-09-7

中文名称

夫罗曲坦琥珀酸盐

SMILES

O=C(O)CCC(O)=O.O=C(C1=CC2=C(NC3=C2C[C@H](NC)CC3)C=C1)N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

Frovatriptan(R)-FrovatriptanSB 209509VML 251SB209509SB-209509VML251VML-2515-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptor5-HT1B5-HT1Dorallymigraine5-HT7carotidvascularmenstrualnauseavomitingphotophobiaphonophobiaInhibitorinhibitorinhibit

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产品名称:
Frovatriptan succinate
目录号:
HY-B1658B
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