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Chemical Compound Review

Alniditan HCl     N-[[(2R)-chroman-2- yl]methyl]-N'-(1,4,5,6...

Synonyms: CHEMBL2105936, R-91274, AC1L32UJ, R-091274, R091274, ...
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Disease relevance of Alniditan

  • Both of these suggestions warrant further and larger trials of alniditan in acute migraine [1].
  • Alniditan was superior to placebo in reducing the associated symptoms of nausea, phonophobia and photophobia, and in increasing patients' functional ability [1].
  • Alniditan produced a slight bradycardia (maximum change: -4 +/- 1%) and a more pronounced hypotensive effect (maximum change: -23 +/- 5%) [2].
  • Iontophoresis slightly increased drug quantities in stratum corneum compared to passive diffusion but it strongly increased alniditan quantities in viable skin. ii) The objective to deliver in vivo 0.5 mg of alniditan within less than 1 h was reached but an erythema was detected at the anode [3].
  • In six animals pre-treated with the potent and selective 5-HT1B/1D receptor antagonist, GR127935, the alniditan-induced changes in carotid haemodynamics were clearly antagonised, whereas the bradycardia and hypotension remained unaffected [2].

High impact information on Alniditan

  • Therefore, in functional assays, the potency of alniditan was much higher at 5-HT1D receptors than at 5-HT1A receptors [4].
  • We investigated the receptor-binding profile in vitro of alniditan compared with sumatriptan and dihydroergotamine for 28 neurotransmitter receptor subtypes, several receptors for peptides and lipid-derived factors, ion channel-binding sites, and monoamine transporters [4].
  • Alniditan revealed nanomolar affinity for calf substantia nigra 5-HT1D and for cloned h5-HT1D alpha, h5-HT1D beta and h5-HT1A receptors (Ki = 0.8, 0.4, 1.1, and 3.8 nM, respectively) [4].
  • In signal transduction assays using cells expressing recombinant h5-HT1D alpha, h5-HT1D beta, or h5-HT1A receptors, alniditan (like 5-HT) was a full agonist for inhibition of stimulated adenylyl cyclase (IC50 = 1.1, 1.3, and 74 nM, respectively, for alniditan) [4].
  • Second, the novel 5-HT1B/D agonists zolmitriptan (311C90), rizatriptan (MK-462), eletriptan (UK-116,044), avitriptan (BMS-180048) and alniditan (R091274) were all proved superior to placebo for attack treatment, but their advantages over sumatriptan are yet to be analysed in more detail [5].

Biological context of Alniditan


Anatomical context of Alniditan


Gene context of Alniditan


Analytical, diagnostic and therapeutic context of Alniditan


  1. Alniditan in the acute treatment of migraine attacks: a subcutaneous dose-finding study. Subcutaneous Alniditan Study Group. Goldstein, J., Dahlöf, C.G., Diener, H.C., Olesen, J., Schellens, R., Senard, J.M., Simard, D., Steiner, T.J. Cephalalgia : an international journal of headache. (1996) [Pubmed]
  2. The antimigraine agent alniditan selectively constricts porcine carotid arteriovenous anastomoses via 5-HT1B/1D receptors. De Vries, P., Willems, E.W., Heiligers, J.P., Villalón, C.M., Saxena, P.R. Eur. J. Pharmacol. (1998) [Pubmed]
  3. Transdermal permeation of alniditan by iontophoresis: in vitro optimization and human pharmacokinetic data. Jadoul, A., Mesens, J., Caers, W., de Beukelaar, F., Crabbé, R., Préat, V. Pharm. Res. (1996) [Pubmed]
  4. Alniditan, a new 5-hydroxytryptamine1D agonist and migraine-abortive agent: ligand-binding properties of human 5-hydroxytryptamine1D alpha, human 5-hydroxytryptamine1D beta, and calf 5-hydroxytryptamine1D receptors investigated with [3H]5-hydroxytryptamine and [3H]alniditan. Leysen, J.E., Gommeren, W., Heylen, L., Luyten, W.H., Van de Weyer, I., Vanhoenacker, P., Haegeman, G., Schotte, A., Van Gompel, P., Wouters, R., Lesage, A.S. Mol. Pharmacol. (1996) [Pubmed]
  5. Acute migraine therapy: the newer drugs. Schoenen, J. Curr. Opin. Neurol. (1997) [Pubmed]
  6. Selective vasoconstriction by alniditan in the carotid vascular bed of anaesthetized dogs. Van de Water, A., D'Aubioul, J., Van Gerven, W., Van Ammel, K., De Clerck, F. Eur. J. Pharmacol. (1996) [Pubmed]
  7. Effects of alniditan on neurogenic oedema in the rat dura mater and on contraction of rat basilar artery. Limmroth, V., Bischoff, A., Fetscher, C., Wermelskirchen, D., Diener, H., Michel, M.C. Eur. J. Pharmacol. (1999) [Pubmed]
  8. Agonistic properties of alniditan, sumatriptan and dihydroergotamine on human 5-HT1B and 5-HT1D receptors expressed in various mammalian cell lines. Lesage, A.S., Wouters, R., Van Gompel, P., Heylen, L., Vanhoenacker, P., Haegeman, G., Luyten, W.H., Leysen, J.E. Br. J. Pharmacol. (1998) [Pubmed]
  9. Transdermal alniditan delivery by skin electroporation. Jadoul, A., Lecouturier, N., Mesens, J., Caers, W., Préat, V. Journal of controlled release : official journal of the Controlled Release Society. (1998) [Pubmed]
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