A 5-HT1F receptor antagonist
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LY344864 (hydrochloride)

Item No. 29496

Technical Information
Formal Name
N-[(3R)-3-(dimethylamino)-2,3,4,9-tetrahydro-1H-carbazol-6-yl]-4-fluoro-benzamide, monohydrochloride
CAS Number
1217756-94-9
Molecular Formula
C21H22FN3O • HCl
Formula Weight
Purity
≥98%
Formulation
A solid
DMF: 3mg/mLDMSO: 10mg/mLDMSO:PBS (pH 7.2) (1:3): 0.25mg/mL
λmax
230, 268 nm
SMILES
CN(C)[C@H](CC1)CC2=C1NC3=CC=C(NC(C4=CC=C(F)C=C4)=O)C=C32
InChi Code
InChI=1S/C21H22FN3O/c1-25(2)16-8-10-20-18(12-16)17-11-15(7-9-19(17)24-20)23-21(26)13-3-5-14(22)6-4-13/h3-7,9,11,16,24H,8,10,12H2,1-2H3,(H,23,26)/t16-/m1/s1
InChi Key
GKWHICIUSVVNGX-MRXNPFEDSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    LY344864 is an agonist of the serotonin (5-HT) receptor subtype 5-HT1F (Ki = 6 nM).1 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).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Phebus, L.A., Johnson, K.W., Zgombick, J.M., et alCharacterization of LY344864 as a pharmacological tool to study 5-HT1F receptors: Binding affinities, brain penetration and activity in the neurogenic dural inflammation model of migraine. Life Sci. 61(21), 2117-2126 (1997).