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Chemical Compound Review

Rapimelt     (4S)-4-[[3-(2- dimethylaminoethyl)-1H- indol...

Synonyms: Zomigoro, Zomigon, AscoTopand, Flezol, Zomig, ...
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Disease relevance of zolmitriptan


Psychiatry related information on zolmitriptan


High impact information on zolmitriptan


Chemical compound and disease context of zolmitriptan


Biological context of zolmitriptan


Anatomical context of zolmitriptan


Associations of zolmitriptan with other chemical compounds

  • Anpirtoline, like other 5-HT1B agonists (CP-94,253, zolmitriptan), decreased both instigated and frustration-heightened aggression, while motor behavior was unaffected [20].
  • Naratriptan tended to increase ASF slope (mean difference 0.23 +/- 0.62 microV/10 dB, p = 0.06) while zolmitriptan (0.08 +/- 0.95 microV/10 dB, p = 0.35) did not [21].
  • In membranes obtained from cells co-expressing the porcine 5-HT(1B) receptor and a mutant G(alphao)Cys(351)Ile protein, 5-HT and zolmitriptan increased, while the 5-HT(1B) receptor antagonist SB224289 decreased basal [(35)S]-GTPgammaS binding, thus showing inverse agonism [22].
  • Thirty healthy subjects received either ASA or ZOL vs. placebo using a double blind cross over design. nBR was recorded in all patients and subjects before, 60 and 90 min after treatment [23].
  • There was a significant increase in serum growth hormone after zolmitriptan compared to placebo, however there were no significant effects on cortisol, prolactin or oral temperature [24].

Gene context of zolmitriptan

  • 4. Primary metabolism of zolmitriptan is dependent mainly on CYP1A2, whereas MAO-A is responsible for further metabolism of N-desmethyl-zolmitriptan, the active metabolite [25].
  • 6. These results show that 311C90, a novel member of the 5-HT1B/1D agonist drug class, exhibits a high degree of pharmacological specificity [26].
  • Zolmitriptan-induced growth hormone release in humans: mediation by 5-HT1D receptors [27]?
  • This suggests that MAO-A is involved in the metabolism of 183C91 and it may be prudent to limit the daily zolmitriptan dose in migraine patients maintained on a MAO-A inhibitor [28].
  • The latency of the P300 ERP was unaffected by zolmitriptan and there was no clinically significant effect on the EEG [29].

Analytical, diagnostic and therapeutic context of zolmitriptan


  1. Clinical efficacy and tolerability of 2.5 mg zolmitriptan for the acute treatment of migraine. The 042 Clinical Trial Study Group. Solomon, G.D., Cady, R.K., Klapper, J.A., Earl, N.L., Saper, J.R., Ramadan, N.M. Neurology (1997) [Pubmed]
  2. Oral zolmitriptan is effective in the acute treatment of cluster headache. Bahra, A., Gawel, M.J., Hardebo, J.E., Millson, D., Breen, S.A., Goadsby, P.J. Neurology (2000) [Pubmed]
  3. 311C90, a new central and peripherally acting 5-HT1D receptor agonist in the acute oral treatment of migraine: a double-blind, placebo-controlled, dose-range finding study. Visser, W.H., Klein, K.B., Cox, R.C., Jones, D., Ferrari, M.D. Neurology (1996) [Pubmed]
  4. Triptans reduce the inflammatory response in bacterial meningitis. Hoffmann, O., Keilwerth, N., Bille, M.B., Reuter, U., Angstwurm, K., Schumann, R.R., Dirnagl, U., Weber, J.R. J. Cereb. Blood Flow Metab. (2002) [Pubmed]
  5. Zolmitriptan: a review of its use in migraine. Spencer, C.M., Gunasekara, N.S., Hills, C. Drugs (1999) [Pubmed]
  6. Decreased sensitivity of 5-HT(1D) receptors in melancholic depression. Whale, R., Clifford, E.M., Bhagwagar, Z., Cowen, P.J. The British journal of psychiatry : the journal of mental science. (2001) [Pubmed]
  7. Lack of an effect of zolmitriptan (Zomig, 311C90) on psychometric task performance: results of a placebo-controlled study in healthy volunteers. Mercer, A.J., Lamb, R.J., Rolan, P.E., Gibbens, M., Posner, J. Psychopharmacology (Berl.) (1998) [Pubmed]
  8. Zolmitriptan (a 5-HT1B/1D receptor agonist with central action) does not increase symptoms in obsessive compulsive disorder. Boshuisen, M.L., den Boer, J.A. Psychopharmacology (Berl.) (2000) [Pubmed]
  9. Efficacy of oral ketoprofen in acute migraine: a double-blind randomized clinical trial. Dib, M., Massiou, H., Weber, M., Henry, P., Garcia-Acosta, S., Bousser, M.G. Neurology (2002) [Pubmed]
  10. Vascular effects of 5-HT1B/1D-receptor agonists in patients with migraine headaches. de Hoon, J.N., Willigers, J.M., Troost, J., Struijker-Boudier, H.A., Van Bortel, L.M. Clin. Pharmacol. Ther. (2000) [Pubmed]
  11. The pharmacodynamics and pharmacokinetics of the 5HT1B/1D-agonist zolmitriptan in healthy young and elderly men and women. Peck, R.W., Seaber, E.J., Dixon, R.M., Layton, G.R., Weatherley, B.C., Jackson, S.H., Rolan, P.E., Posner, J. Clin. Pharmacol. Ther. (1998) [Pubmed]
  12. 311C90: long-term efficacy and tolerability profile for the acute treatment of migraine. International 311C90 Long-Term Study Group. Zagami, A.S. Neurology (1997) [Pubmed]
  13. Serotonin 5HT1B/1D receptor agonists abolish NMDA receptor-evoked enhancement of nitric oxide synthase activity and cGMP concentration in brain cortex slices. Stepień, A., Chalimoniuk, M., Strosznajder, J. Cephalalgia : an international journal of headache. (1999) [Pubmed]
  14. Comparison of rizatriptan 10 mg vs. zolmitriptan 2.5 mg in the acute treatment of migraine. Rizatriptan-Zolmitriptan Study Group. Pascual, J., Vega, P., Diener, H.C., Allen, C., Vrijens, F., Patel, K. Cephalalgia : an international journal of headache. (2000) [Pubmed]
  15. Comparative efficacy of eletriptan and zolmitriptan in the acute treatment of migraine. Steiner, T.J., Diener, H.C., MacGregor, E.A., Schoenen, J., Muirheads, N., Sikes, C.R. Cephalalgia : an international journal of headache. (2003) [Pubmed]
  16. The impact of different antimigraine compounds on platelet and erythrocyte aggregation. Evers, S., Heuel, T., Frese, A., Akova-Oztürk, E., Husstedt, I.W. Cephalalgia : an international journal of headache. (2006) [Pubmed]
  17. Inhibition of trigeminal neurons by intravenous administration of the serotonin (5HT)1B/D receptor agonist zolmitriptan (311C90): are brain stem sites therapeutic target in migraine? Goadsby, P.J., Hoskin, K.L. Pain (1996) [Pubmed]
  18. Effects of the serotonin1B/1D receptor agonist zolmitriptan on motor cortical excitability in humans. Werhahn, K.J., Förderreuther, S., Straube, A. Neurology (1998) [Pubmed]
  19. Pre-clinical pharmacology of zolmitriptan (Zomig; formerly 311C90), a centrally and peripherally acting 5HT1B/1D agonist for migraine. Martin, G.R. Cephalalgia : an international journal of headache. (1997) [Pubmed]
  20. Aggression escalated by social instigation or by discontinuation of reinforcement ("frustration") in mice: inhibition by anpirtoline: a 5-HT1B receptor agonist. de Almeida, R.M., Miczek, K.A. Neuropsychopharmacology (2002) [Pubmed]
  21. Auditory evoked potentials in the assessment of central nervous system effects of antimigraine drugs. Roon, K.I., Sándor, P.S., Schoonman, G.G., Lamers, F.P., Schoenen, J., Ferrari, M.D., van Dijk, J.G. Cephalalgia : an international journal of headache. (1999) [Pubmed]
  22. Molecular cloning, pharmacological properties and tissue distribution of the porcine 5-HT(1B) receptor. Bhalla, P., Sharma, H.S., Ma, X., Wurch, T., Pauwels, P.J., Saxena, P.R. Br. J. Pharmacol. (2001) [Pubmed]
  23. Differences of anti-nociceptive mechanisms of migraine drugs on the trigeminal pain processing during and outside acute migraine attacks. Katsarava, Z., Limmroth, V., Baykal, O., Akguen, D., Diener, H.C., Kaube, H. Cephalalgia : an international journal of headache. (2004) [Pubmed]
  24. Low dose zolmitriptan as a 5-HT neuroendocrine challenge agent in humans. Moeller, F.G., Bjork, J.M., Dougherty, D.M., Van de Kar, L.D., Marsh, D.M., Swann, A.C. Psychoneuroendocrinology (2000) [Pubmed]
  25. Determination of the human cytochrome P450 isoforms involved in the metabolism of zolmitriptan. Wild, M.J., McKillop, D., Butters, C.J. Xenobiotica (1999) [Pubmed]
  26. Receptor specificity and trigemino-vascular inhibitory actions of a novel 5-HT1B/1D receptor partial agonist, 311C90 (zolmitriptan). Martin, G.R., Robertson, A.D., MacLennan, S.J., Prentice, D.J., Barrett, V.J., Buckingham, J., Honey, A.C., Giles, H., Moncada, S. Br. J. Pharmacol. (1997) [Pubmed]
  27. Zolmitriptan-induced growth hormone release in humans: mediation by 5-HT1D receptors? Whale, R., Bhagwagar, Z., Cowen, P.J. Psychopharmacology (Berl.) (1999) [Pubmed]
  28. Potential drug interactions with the novel antimigraine compound zolmitriptan (Zomig, 311C90). Rolan, P. Cephalalgia : an international journal of headache. (1997) [Pubmed]
  29. Effects of zolmitriptan (Zomig) on central serotonergic neurotransmission as assessed by active oddball auditory event-related potentials in volunteers without migraine. Hughes, A.M., Dixon, R., Dane, A., Kemp, J., Cummings, L., Yates, R.A. Cephalalgia : an international journal of headache. (1999) [Pubmed]
  30. Effectiveness of Intranasal Zolmitriptan in Acute Cluster Headache: A Randomized, Placebo-Controlled, Double-blind Crossover Study. Cittadini, E., May, A., Straube, A., Evers, S., Bussone, G., Goadsby, P.J. Arch. Neurol. (2006) [Pubmed]
  31. Clinical applications of zolmitriptan (Zomig, 311C90). Lipton, R.B., Stewart, W.F. Cephalalgia : an international journal of headache. (1997) [Pubmed]
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