A 5-HT1F receptor agonist (Ki = 6 nM); selective for 5-HT1F over 5-HT1A-E

LY344864 (hydrochloride) – 25 mg

Brand:
Cayman
CAS:
1217756-94-9
Storage:
-20
UN-No:
Non-Hazardous - /

LY344864 is an agonist of the serotonin (5-HT) receptor subtype 5-HT1F (Ki = 6 nM).{53306} It is selective for 5-HT1F over 5-HT1A-E , 5-HT2A-C, and 5-HT7 receptors (Kis = 0.53-4.85 µM), as well as dopamine D1 and D2, GABAA, histamine H1, muscarinic, and α1-, α2-, and β-adrenergic receptors with Ki values ranging from 3.69 to greater than 100 µM. LY344864 inhibits forskolin-induced cAMP accumulation in L-M(TK-) cells expressing recombinant human 5-HT1F receptors with an EC50 value of 3 nM. It decreases electrically stimulated extravasation of plasma proteins in the dura mater in a rat trigeminal nerve model of migraine headache (ID50s = 0.6 and 2.1 ng/kg for i.v. and oral administration, respectively).  

 

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SKU: 29496 - 25 mg Category:

Description

A 5-HT1F receptor agonist (Ki = 6 nM); selective for 5-HT1F over 5-HT1A-E , 5-HT2A-C, and 5-HT7 receptors (Kis = 0.53-4.85 µM), as well as dopamine D1 and D2, GABAA, histamine H1, muscarinic, and α1-, α2-, and β-adrenergic receptors (Kis = 3.69->100 µM); inhibits forskolin-stimulated cAMP accumulation in L-M(TK-) cells expressing recombinant human 5-HT1F receptors (EC50 = 3 nM); decreases electrically stimulated extravasation of plasma proteins in the dura mater in a rat trigeminal nerve model of migraine headache (ID50s = 0.6 and 2.1 ng/kg for i.v. and oral administration, respectively)

Formal name: N-[(3R)-3-(dimethylamino)-2,3,4,9-tetrahydro-1H-carbazol-6-yl]-4-fluoro-benzamide, monohydrochloride

Synonyms: 

Molecular weight: 387.9

CAS: 1217756-94-9

Purity: ≥98%

Formulation: A solid

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