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Chemical Compound Review:

AC1NSKBH 4-fluoro-N-[3-(1-methyl-4- piperidyl)-1H...

Synonyms: CHEMBL101690, SureCN6911508, CHEBI:270328, DNC005161, LY-334370, ...

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Disease relevance of LY334370

Selective seratonin 1F (5-HT(1F)) receptor agonist LY334370 for acute migraine: a randomised controlled trial [1].
More patients given LY334370 than placebo reported asthenia, somnolence, and dizziness [1].

High impact information on LY334370

We have studied the efficacy of LY334370, a selective serotonin 1F (5-HT(1F)) receptor agonist with preclinical efficacy and no vasoconstriction, for migraine relief [1].
Contractile responses to ergotamine, sumatriptan and the novel 5-HT(1F) receptor agonists, LY334370 and LY344864 were examined using the rabbit saphenous vein [2].
Possible antimigraine mechanisms of action of the 5HT1F receptor agonist LY334370 [3].
G-protein activation at 5-HT1A receptors by the 5-ht1F ligand LY334370 in guinea-pig brain sections and recombinant cell lines [4].
3. Application of LY334370 (10 microM) to guinea-pig brain sections resulted in an increase of [35S]-GTPgammaS binding in hippocampus (123+/-17%), lateral septum (58+/-14%), dorsal raphe (57+/-10%), entorhinal (37+/-11%) and cingulate cortex (28+/-10%) [4].

Chemical compound and disease context of LY334370

(iv) Selective 5-HT1F receptor agonists (LY334370; LY344864) are effective in preclinical migraine models and are non-vasoconstrictive [5].

Anatomical context of LY334370

The selective 5-HT(1F) receptor agonists, LY334370 or LY344864 (up to 10(-4) M), did not contract the rabbit saphenous vein [2].
6. In conclusion, in guinea-pig brain sections and recombinant cell lines the 5-ht1F receptor agonist LY334370 causes G-protein activation that is mediated by 5-HT1A receptors [4].
5. The maximal LY334370-induced [35S]-GTPgammaS binding response (83 to 94%) in membranes of recombinant C6-glial/h 5-HT1A and HeLa/h 5-HT1A cells was close to that of 5-HT, suggesting LY334370 to exert high intrinsic activity at h 5-HT1A receptors [4].

Gene context of LY334370

The 5-HT1F receptor ligand LY334370 (4-fluoro-N-[3-(1-methyl-4-piperidinyl)-1H-indol-5-yl]-benzamide) was the most potent compound tested with an EC50 of 2.13 +/- 0.15 nM [6].

References

Selective seratonin 1F (5-HT(1F)) receptor agonist LY334370 for acute migraine: a randomised controlled trial. Goldstein, D.J., Roon, K.I., Offen, W.W., Ramadan, N.M., Phebus, L.A., Johnson, K.W., Schaus, J.M., Ferrari, M.D. Lancet (2001) [Pubmed]
Contractile responses to sumatriptan and ergotamine in the rabbit saphenous vein: effect of selective 5-HT(1F) receptor agonists and PGF(2alpha). Cohen, M.L., Schenck, K. Br. J. Pharmacol. (2000) [Pubmed]
Possible antimigraine mechanisms of action of the 5HT1F receptor agonist LY334370. Shepheard, S., Edvinsson, L., Cumberbatch, M., Williamson, D., Mason, G., Webb, J., Boyce, S., Hill, R., Hargreaves, R. Cephalalgia : an international journal of headache. (1999) [Pubmed]
G-protein activation at 5-HT1A receptors by the 5-ht1F ligand LY334370 in guinea-pig brain sections and recombinant cell lines. Dupuis, D.S., Colpaert, F.C., Pauwels, P.J. Br. J. Pharmacol. (1998) [Pubmed]
5-HT1F receptor agonists in acute migraine treatment: a hypothesis. Ramadan, N.M., Skljarevski, V., Phebus, L.A., Johnson, K.W. Cephalalgia : an international journal of headache. (2003) [Pubmed]
Human 5-HT1F receptor-stimulated [35S]GTPgammaS binding: correlation with inhibition of guinea pig dural plasma protein extravasation. Wainscott, D.B., Johnson, K.W., Phebus, L.A., Schaus, J.M., Nelson, D.L. Eur. J. Pharmacol. (1998) [Pubmed]

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