Date published: 2025-10-16

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L-694,247 (CAS 137403-12-4)

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Alternate Names:
2-[5-[3-(4-Methylsulfonylamino)benzyl-1,2,4-oxadiazol-5-yl]-1H-indol-3-yl]ethanamine
Application:
L-694,247 is a highly potent and selective SR-1D agonist
CAS Number:
137403-12-4
Molecular Weight:
411.48
Molecular Formula:
C20H21N5O3S
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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L-694,247 is a member of tryptamines. It is known to be a highly potent and selective serotonin (5-HT) receptor SR-1D agonist, as well as an activator of SR-1B. 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 and potassium-induced 5-HT release. It also induces a partial blockade of water intake.


L-694,247 (CAS 137403-12-4) References

  1. On the role of 5-HT1B/1D receptors in modulating transmission in a spinal reflex pathway in the decerebrated rabbit.  |  Ogilvie, J., et al. 1999. Br J Pharmacol. 128: 781-7. PMID: 10516662
  2. Hypothalamic paraventricular 5-hydroxytryptamine: receptor-specific inhibition of NPY-stimulated eating and energy metabolism.  |  Currie, PJ., et al. 2002. Pharmacol Biochem Behav. 71: 709-16. PMID: 11888562
  3. Vasodilator and vasoconstrictor responses induced by 5-hydroxytryptamine in the in situ blood autoperfused hindquarters of the anaesthetized rat.  |  Calama, E., et al. 2002. Naunyn Schmiedebergs Arch Pharmacol. 366: 110-6. PMID: 12122496
  4. 5-Hydroxytryptamine-induced vasodilator responses in the hindquarters of the anaesthetized rat, involve beta2-adrenoceptors.  |  Calama, E., et al. 2003. J Pharm Pharmacol. 55: 1371-8. PMID: 14607019
  5. In vivo effects of local activation and blockade of 5-HT1B receptors on globus pallidus neuronal spiking.  |  Querejeta, E., et al. 2005. Brain Res. 1043: 186-94. PMID: 15862532
  6. The role of endothelium-derived hyperpolarizing factor and cyclooxygenase pathways in the inhibitory serotonergic response to the pressor effect elicited by sympathetic stimulation in chronic sarpogrelate treated rats.  |  García-Pedraza, JÁ., et al. 2014. Eur J Pharmacol. 731: 80-7. PMID: 24675150
  7. Pharmacological evidence that 5-HT1D activation induces renal vasodilation by NO pathway in rats.  |  García-Pedraza, JÁ., et al. 2015. Clin Exp Pharmacol Physiol. 42: 640-7. PMID: 25854421
  8. 5-HT1D receptor inhibits renal sympathetic neurotransmission by nitric oxide pathway in anesthetized rats.  |  García-Pedraza, JÁ., et al. 2015. Vascul Pharmacol. 72: 172-80. PMID: 26003124
  9. 5-HT2 receptor blockade exhibits 5-HT vasodilator effects via nitric oxide, prostacyclin and ATP-sensitive potassium channels in rat renal vasculature.  |  García-Pedraza, JA., et al. 2016. Vascul Pharmacol. 79: 51-59. PMID: 26586311
  10. 5-HT modulates the rat mesenteric vasopressor outflow by 5-HT1D sympatholytic receptors.  |  García-Pedraza, JÁ., et al. 2017. Clin Exp Pharmacol Physiol. 44: 1224-1231. PMID: 28771848
  11. Sumatriptan inhibits the electrophysiological activity of ASICs in rat trigeminal ganglion neurons.  |  Guo, L., et al. 2018. Eur J Pharmacol. 841: 98-103. PMID: 30336137
  12. Fluoxetine Treatment Decreases Cardiac Vagal Input and Alters the Serotonergic Modulation of the Parasympathetic Outflow in Diabetic Rats.  |  García-Domingo, M., et al. 2022. Int J Mol Sci. 23: PMID: 35628547
  13. Evidence for presynaptic location of inhibitory 5-HT1D beta-like autoreceptors in the guinea-pig brain cortex.  |  Bühlen, M., et al. 1996. Naunyn Schmiedebergs Arch Pharmacol. 353: 281-9. PMID: 8692282
  14. Effect of third ventricle administration of L-694,247, a selective 5-HT1D receptor agonist, on water intake in rats.  |  De Castro-e-Silva, E., et al. 1997. Pharmacol Biochem Behav. 57: 749-54. PMID: 9259002
  15. Characterization of prejunctional 5-HT1 receptors that mediate the inhibition of pressor effects elicited by sympathetic stimulation in the pithed rat.  |  Morán, A., et al. 1998. Br J Pharmacol. 123: 1205-13. PMID: 9559906

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

L-694,247, 10 mg

sc-361223
10 mg
$195.00

L-694,247, 50 mg

sc-361223A
50 mg
$803.00