CAS:181183-52-8 Almotriptan (malate);PNU180638 线路优化
作者:zhn
发布时间:2024-04-03
16:45:24
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产品名称:CAS:181183-52-8 Almotriptan (malate);PNU180638 线路优化
产品描述:
Product Name:Almotriptan (malate)
Synonyms:PNU180638
CAS Number:181183-52-8
M. Wt:469.55
Target:5-HT Receptor
Pathway:GPCR/G Protein; Neuronal Signaling
Approved Type:FDA
Biological Activity:Almotriptan Malate is a 5-HT1B/1D-receptor agonist used to treat migraine.
IC50:
Target: 5-hydroxytryptamine1B/1D (5-HT1B/1D) Receptor
Almotriptan Malate is a selective 5-hydroxytryptamine1B/1D (5-HT1B/1D) receptor agonist, used for the treatment of Migraine attacks in adults. Almotriptan showed low nanomolar affinity for the 5-HT(1B) and 5-HT(1D) receptors in several species, including the human, while affinity for 5-HT receptors other than 5-HT(1B/1D) was clearly less. Almotriptan did not exhibit significant affinity for several non-5-HT receptors studied up to 100 microM. Almotriptan inhibited forskolin-stimulated cyclic AMP accumulation in HeLa cells transfected with 5-HT(1B) or 5-HT(1D) human receptors [1]. Almotriptan had a mild antiemetic effect and a slight, transient diuretic effect in dogs, although the latter effect is probably of no clinical relevance. In addition, no effect on the respiratory system of conscious guinea pigs was observed following almotriptan treatment. These results indicate that almotriptan has a favourable safety profile with respect to the central nervous, renal and respiratory systems [2].
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