A 5-HT1D receptor agonist
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L-694,247 (trifluoroacetate salt)

Item No. 40639

Technical Information
Formal Name
N-[4-[[5-[3-(2-aminoethyl)-1H-indol-5-yl]-1,2,4-oxadiazol-3-yl]methyl]phenyl]-methanesulfonamide, trifluoroacetate salt
Molecular Formula
C20H21N5O3S • XCF3COOH
Formula Weight
Purity
≥95%
Formulation
A crystalline solid
Acetonitrile: Slightly soluble: 0.1-1 mg/mlWater: Sparingly soluble: 1-10 mg/ml
SMILES
NCCC1=CNC(C=C2)=C1C=C2C3=NC(CC4=CC=C(NS(C)(=O)=O)C=C4)=NO3.FC(F)(F)C(O)=O
InChi Code
InChI=1S/C20H21N5O3S.C2HF3O2/c1-29(26,27)25-16-5-2-13(3-6-16)10-19-23-20(28-24-19)14-4-7-18-17(11-14)15(8-9-21)12-22-18;3-2(4,5)1(6)7/h2-7,11-12,22,25H,8-10,21H2,1H3;(H,6,7)
InChi Key
UPFZBIGQSZGYJJ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    Product Description

    L-694,247 is an agonist of the serotonin (5-HT) receptor subtype 5-HT1D.1 It is selective for 5-HT1D over the 5-HT1A, 5-HT1C, 5-HT1E, 5-HT2, and 5-HT3 receptors (Kis = 0.093, 2.29, 380, 2,187, 316, and >10,000 nM, respectively). L-694,247 inhibits adenylyl cyclase activity induced by forskolin (Item No. 11018) in guinea pig substantia nigra homogenates and potassium-induced 5-HT release in isolated guinea pig frontal cortex strips (EC50s = 0.79 and 0.4 nM, respectively). It decreases water intake in dehydrated rats as well as prevents carbachol-, angiotensin II-, or isoproterenol-induced increases in water intake in normohydrated rats in a dose-dependent manner.2 Intra-atrial administration of L-694,247 (0.00000125-0.1 µg/kg) decreases renal perfusion pressure but does not affect systolic blood pressure or heart rate in in situ autoperfused rat kidney infused with phenylephrine (Item Nos. 17205 | 18619).3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Beer, M.S., Stanton, J.A., Bevan, Y., et alL-694,247: A potent 5-HT1D receptor agonist. Br. J. Pharmacol. 110(3), 1196-1200 (1993).

    2. De Castro-e-Silva, E., Sarmento, C., Nascimento, T.A., et alEffect of third ventricle administration of L-694,247, a selective 5-HT1D receptor agonist, on water intake in rats. Pharmacol. Biochem. Behav. 57(4), 749-754 (1997).

    3. García-Pedraza, J.Á., García, M., Martín, M.L., et alPharmacological evidence that 5-HT1D activation induces renal vasodilation by NO pathway in rats. Clin. Exp. Pharmacol. Physiol. 42(6), 640-647 (2015).