An agonist of 5-HT1B and 5-HT1D receptors (IC50s = 12 and 13 nM

Almotriptan (malate) – 5 mg

Brand:
Cayman
CAS:
181183-52-8
Storage:
-20
UN-No:
Non-Hazardous - /

Almotriptan is an agonist of the serotonin (5-HT) receptor subtypes 5-HT1B and 5-HT1D (IC50s = 12 and 13 nM, respectively, in a radioligand binding assay).{47183} It is selective for human 5-HT1B and 5-HT1D receptors over rat 5-HT1A and human 5-HT2A and 5-HT4 receptors (IC50s = 0.85, 25.1, and 140 μM, respectively). Almotriptan induces contractions in isolated canine saphenous veins (EC50 = 394 nM) but not isolated rabbit renal or mesenteric arteries. It increases carotid vascular resistance in anesthetized cats (ED100 = 11 μg/kg, i.v.) without increasing blood pressure or heart rate.{47184} Formulations containing almotriptan have been used in the treatment of migraine headaches.  

 

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Description

An agonist of 5-HT1B and 5-HT1D receptors (IC50s = 12 and 13 nM, respectively, in a radioligand binding assay); selective for human 5-HT1B and 5-HT1D receptors over rat 5-HT1A and human 5-HT2A and 5-HT4 receptors (IC50s = 0.85, 25.1, and 140 μM, respectively); induces contractions in isolated canine saphenous veins (EC50 = 394 nM) but not isolated rabbit renal or mesenteric arteries; increases carotid vascular resistance in anesthetized cats (ED100 = 11 μg/kg, i.v.) without increasing blood pressure or heart rate

Formal name: 2-hydroxy-butanedioic acid, compd. with N,N-dimethyl-5-[(1-pyrrolidinylsulfonyl)methyl]-1H-indole-3-ethanamine

Synonyms:  PNU 180638E

Molecular weight: 469.6

CAS: 181183-52-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Cardiovascular System|Cardiovascular Diseases||Research Area|Cardiovascular System|Vasculature|Vasoconstriction||Research Area|Neuroscience|Pain Research

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