Eletriptan HBr

  • CAT Number: A001182
  • CAS Number: 177834-92-3
  • Molecular Formula: C22H27BrN2O2S
  • Molecular Weight: 463.43
  • Purity: ≥95%
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Eletriptan Hydrobromide is a triptan with specific affinity for the 5-hydroxytriptamine1B/1D receptor. Eletriptan hydrobromide binds to and acts at serotonin 5-HT1B receptors located on intracranial blood vessels which leads to vasoconstriction. This drug may also exert its effects by binding to and activating 5-HT 1D receptors on sensory nerve endings in the trigeminal system, which results in the inhibition of pro-inflammatory neuropeptide release. Eletriptan hydrobromide is used to relieve pain or symptoms associated with migraine headaches.

Catalog Number A001182
CAS Number 177834-92-3
Synonyms

UK-116044

Molecular Formula

C22H27BrN2O2S

Purity 95%
Target 5-HT Receptor
Solubility Soluble in DMSO > 10 mM
Storage 3 years -20C powder
Reference

</br>1: Madasu SB, Vekariya NA, Kiran MN, Gupta B, Islam A, Douglas PS, Babu KR.</br> Synthesis of compounds related to the anti-migraine drug eletriptan hydrobromide.</br> Beilstein J Org Chem. 2012;8:1400-5. Epub 2012 Aug 30. PubMed PMID: 23019477;</br> PubMed Central PMCID: PMC3458767.</br>2: Landy SH, Tepper SJ, Schweizer E, Almas M, Ramos E. Outcome for headache and</br> pain-free nonresponders to treatment of the first attack: a pooled post-hoc</br> analysis of four randomized trials of eletriptan 40 mg. Cephalalgia. 2014</br> Apr;34(5):376-81. doi: 10.1177/0333102413512035. Epub 2013 Nov 21. PubMed PMID:</br> 24265285.</br>3: Bhambri R, Mardekian J, Liu LZ, Schweizer E, Ramos E. A review of the</br> pharmacoeconomics of eletriptan for the acute treatment of migraine. Int J Gen</br> Med. 2015 Jan 12;8:27-36. doi: 10.2147/IJGM.S73673. eCollection 2015. Review.</br> PubMed PMID: 25624770; PubMed Central PMCID: PMC4296958.</br>4: Kertesz DP, Trabekin O, Vanetik MS. Headache treatment after electroconvulsive</br> treatment: a single-blinded trial comparator between eletriptan and paracetamol. </br> J ECT. 2015 Jun;31(2):105-9. doi: 10.1097/YCT.0000000000000179. PubMed PMID:</br> 25181019.</br>5: Bhambri R, Martin VT, Abdulsattar Y, Silberstein S, Almas M, Chatterjee A,</br> Ramos E. Comparing the efficacy of eletriptan for migraine in women during</br> menstrual and non-menstrual time periods: a pooled analysis of randomized</br> controlled trials. Headache. 2014 Feb;54(2):343-54. doi: 10.1111/head.12257. Epub</br> 2013 Oct 29. PubMed PMID: 24256184.</br>6: Almas M, Tepper SJ, Landy S, Schweizer E, Ramos E. Consistency of eletriptan</br> in treating migraine: Results of a randomized, within-patient multiple-dose</br> study. Cephalalgia. 2014 Feb;34(2):126-35. doi: 10.1177/0333102413500726. Epub</br> 2013 Aug 14. PubMed PMID: 23946318.</br>7: Dias A, Franco E, Hebert K, Mercedes A. Myocardial infarction after taking</br> eletriptan. Rev Port Cardiol. 2014 Jul-Aug;33(7-8):475.e1-3. doi:</br> 10.1016/j.repc.2014.03.005. Epub 2014 Aug 23. English, Portuguese. PubMed PMID:</br> 25155004.</br>8: Jocić B, Zecević M, Zivanović L, Protić A, Jadranin M, Vajs V. Study of forced</br> degradation behavior of eletriptan hydrobromide by LC and LC-MS and development</br> of stability-indicating method. J Pharm Biomed Anal. 2009 Nov 1;50(4):622-9. doi:</br> 10.1016/j.jpba.2009.01.034. Epub 2009 Feb 6. PubMed PMID: 19250786.</br>9: Yilmaz H, Kaya M, Ozbek M, Delibasi T. A case of hyperprolactinemia, probably </br> induced by eletriptan. Int J Clin Pharmacol Ther. 2012 Dec;50(12):907-8. doi:</br> 10.5414/CP201744. PubMed PMID: 22943929.</br>10: Ponnuru VS, Challa BR, Nadendla R. Quantitative analysis of eletriptan in</br> human plasma by HPLC-MS/MS and its application to pharmacokinetic study. Anal</br> Bioanal Chem. 2011 Nov;401(8):2539-48. doi: 10.1007/s00216-011-5341-4. Epub 2011 </br> Sep 3. PubMed PMID: 21892641.</br>11: Marcus DA, Bernstein CD, Sullivan EA, Rudy TE. Perimenstrual eletriptan</br> prevents menstrual migraine: an open-label study. Headache. 2010</br> Apr;50(4):551-62. doi: 10.1111/j.1526-4610.2010.01628.x. Epub 2010 Mar 2. PubMed </br> PMID: 20236337.</br>12: Sandrini G, Perrotta A, Tassorelli C, Nappi G. Eletriptan. Expert Opin Drug</br> Metab Toxicol. 2009 Dec;5(12):1587-98. doi: 10.1517/17425250903410226. Review.</br> PubMed PMID: 19929447.</br>13: Sakai Y, Nishikawa M, Diksic M, Aubé M. α-[11C] methyl-L tryptophan-PET as a </br> surrogate for interictal cerebral serotonin synthesis in migraine without aura.</br> Cephalalgia. 2014 Mar;34(3):165-73. doi: 10.1177/0333102413506126. Epub 2013 Sep </br> 20. PubMed PMID: 24057438.</br>14: Pascual J, Leira R, Lainez JM, Liaño H, Díez-Tejedor E, Navarro A, Jiménez D,</br> Ezpeleta D, Mateos V, Madrigal M, Palacios G; Grupo de Investigadores con</br> Eletriptán en España. [Spanish contribution to the clinical development of</br> eletriptan: an analysis of controlled studies]. Neurologia. 2004 Oct;19(8):414-9.</br> Spanish. PubMed PMID: 15470580.</br>15: Sheftell F, Ryan R, Pitman V; Eletriptan Steering Committee. Efficacy,</br> safety, and tolerability of oral eletriptan for treatment of acute migraine: a</br> multicenter, double-blind, placebo-controlled study conducted in the United</br> States. Headache. 2003 Mar;43(3):202-13. PubMed PMID: 12603638.</br>16: Sandrini G, Färkkilä M, Burgess G, Forster E, Haughie S; Eletriptan Steering </br> Committee. Eletriptan vs sumatriptan: a double-blind, placebo-controlled,</br> multiple migraine attack study. Neurology. 2002 Oct 22;59(8):1210-7. PubMed PMID:</br> 12391349.</br>17: Stark R, Dahlöf C, Haughie S, Hettiarachchi J; Eletriptan Steering Committee.</br> Efficacy, safety and tolerability of oral eletriptan in the acute treatment of</br> migraine: results of a phase III, multicentre, placebo-controlled study across</br> three attacks. Cephalalgia. 2002 Feb;22(1):23-32. PubMed PMID: 11993610.</br>18: Diener HC, Jansen JP, Reches A, Pascual J, Pitei D, Steiner TJ; Eletriptan</br> and Cafergot Comparative Study Group. Efficacy, tolerability and safety of oral</br> eletriptan and ergotamine plus caffeine (Cafergot) in the acute treatment of</br> migraine: a multicentre, randomised, double-blind, placebo-controlled comparison.</br> Eur Neurol. 2002;47(2):99-107. PubMed PMID: 11844898.</br>19: Winner P, Linder SL, Lipton RB, Almas M, Parsons B, Pitman V. Eletriptan for </br> the acute treatment of migraine in adolescents: results of a double-blind,</br> placebo-controlled trial. Headache. 2007 Apr;47(4):511-8. PubMed PMID: 17445100.</br>20: McCormack PL, Keating GM. Eletriptan: a review of its use in the acute</br> treatment of migraine. Drugs. 2006;66(8):1129-49. Review. PubMed PMID: 16789799.</br></br>

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