Betahistine free base
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 326652

CAS#: 5638-76-6 (free base)

Description: Betahistine is a histamine analog and H1 receptor agonist that serves as a vasodilator. It is used in MENIERE DISEASE and in vascular headaches but may exacerbate bronchial asthma and peptic ulcers. Betahistine dihydrochloride is an anti-vertigo drug. It is commonly prescribed for balance disorders or to alleviate vertigo symptoms associated with Ménière's disease. It was first registered in Europe in 1970 for the treatment of Ménière's disease.

Chemical Structure

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Betahistine free base
CAS# 5638-76-6 (free base)
Instruction

Theoretical Analysis

MedKoo Cat#: 326652
Name: Betahistine free base
CAS#: 5638-76-6 (free base)
Chemical Formula: C8H12N2
Exact Mass: 136.10
Molecular Weight: 136.198
Elemental Analysis: C, 70.55; H, 8.88; N, 20.57

Price and Availability

Size Price Availability Quantity
500mg USD 90 2 weeks
1g USD 150 2 weeks
2g USD 250 2 weeks
5g USD 350 2 weeks
10g USD 450 2 weeks
20g USD 550 2 weeks
50g USD 750 2 weeks
Bulk inquiry

Synonym: BRN0112294; BRN-0112294; BRN 0112294; beta-Histine; Betahistine; NSC 42617; PT 9 base; Serc base; Sinmenier (free base); Vasomotal. brand names Veserc, Serc, Hiserk, Betaserc, Vergo.

IUPAC/Chemical Name: N-methyl-2-(pyridin-2-yl)ethan-1-amine

InChi Key:

InChi Code:

SMILES Code: CNCCC1=NC=CC=C1

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info: Related: 5638-76-6 (Betahistine free base) 5579-84-0 (Betahistine HCl)

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 136.20 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Albu S, Nagy A, Doros C, Marceanu L, Cozma S, Musat G, Trabalzini F. Treatment of Meniere's disease with intratympanic dexamethazone plus high dosage of betahistine. Am J Otolaryngol. 2016 May-Jun;37(3):225-30. doi: 10.1016/j.amjoto.2015.12.007. Epub 2015 Dec 30. PubMed PMID: 27178513.

2: Yi C, Wenping X, Hui X, Xin H, Xiue L, Jun Z, Shangyong G. Efficacy and acceptability of oxcarbazepine vs. carbamazepine with betahistine mesilate tablets in treating vestibular paroxysmia: a retrospective review. Postgrad Med. 2016 Apr 18:1-4. [Epub ahead of print] PubMed PMID: 27056408.

3: Barak N, Beck Y, Albeck JH. A Randomized, Double-Blind, Placebo-Controlled Pilot Study of Betahistine to Counteract Olanzapine-Associated Weight Gain. J Clin Psychopharmacol. 2016 Jun;36(3):253-6. doi: 10.1097/JCP.0000000000000489. PubMed PMID: 27028981.

4: Chen YY, Chen W, Zhang Q, Li H, Zhang YW, Kang Q, Lan YI, Wu Q. Puerarin and betahistine treatment of vertebrobasilar ischemia vertigo: A meta-analysis of randomized controlled trials. Exp Ther Med. 2016 Mar;11(3):1051-1058. Epub 2016 Jan 18. PubMed PMID: 26998036; PubMed Central PMCID: PMC4774609.

5: Lian J, Huang XF, Pai N, Deng C. Ameliorating antipsychotic-induced weight gain by betahistine: Mechanisms and clinical implications. Pharmacol Res. 2016 Apr;106:51-63. doi: 10.1016/j.phrs.2016.02.011. Epub 2016 Feb 15. Review. PubMed PMID: 26892184.

6: Barak N, Beck Y, Albeck JH. Betahistine decreases olanzapine-induced weight gain and somnolence in humans. J Psychopharmacol. 2016 Mar;30(3):237-41. doi: 10.1177/0269881115626349. Epub 2016 Feb 2. PubMed PMID: 26839321.

7: Seyed Tootoonchi SJ, Ghiasi S, Shadara P, Samani SM, Fouladi DF. Hearing function after betahistine therapy in patients with Ménière's disease. Braz J Otorhinolaryngol. 2015 Dec 18. pii: S1808-8694(15)00234-7. doi: 10.1016/j.bjorl.2015.08.021. [Epub ahead of print] PubMed PMID: 26810620.

8: Adrion C, Fischer CS, Wagner J, Gürkov R, Mansmann U, Strupp M; BEMED Study Group. Efficacy and safety of betahistine treatment in patients with Meniere's disease: primary results of a long term, multicentre, double blind, randomised, placebo controlled, dose defining trial (BEMED trial). BMJ. 2016 Jan 21;352:h6816. doi: 10.1136/bmj.h6816. PubMed PMID: 26797774; PubMed Central PMCID: PMC4721211.

9: Harcourt J, Cosentino S. Betahistine for Meniere's disease. BMJ. 2016 Jan 21;352:i46. doi: 10.1136/bmj.i46. PubMed PMID: 26794224.

10: Betahistine: hallucinations? Prescrire Int. 2015 Nov;24(165):269. PubMed PMID: 26688903.

11: Cho JS, Kim EJ, Lee JH, Kim SY, Kim JM, Byun JI, Nam EJ, Koo BN. Betahistine reduces postoperative nausea and vomiting and dizziness after laparoscopic gynecological surgery. Minerva Anestesiol. 2015 Nov 17. [Epub ahead of print] PubMed PMID: 26576858.

12: Ramos Alcocer R, Ledezma Rodríguez JG, Navas Romero A, Cardenas Nuñez JL, Rodríguez Montoya V, Deschamps JJ, Liviac Ticse JA. Use of betahistine in the treatment of peripheral vertigo. Acta Otolaryngol. 2015 Dec;135(12):1205-11. doi: 10.3109/00016489.2015.1072873. Epub 2015 Aug 6. PubMed PMID: 26245698.

13: Yılmaz H, Aydın S, Sanlı A, Erdoğan BA, Kibar S, Şirvancı S, Kıran D. Evaluation of the Effect of Betahistine on Noise-Induced Hearing Loss Using Distortion Product Otoacoustic Emission and Scanning Electron Microscopy. J Int Adv Otol. 2015 Apr;11(1):6-11. doi: 10.5152/iao.2015.368. PubMed PMID: 26223710.

14: Liu X, Lian J, Hu CH, Deng C. Betahistine co-treatment ameliorates dyslipidemia induced by chronic olanzapine treatment in rats through modulation of hepatic AMPKα-SREBP-1 and PPARα-dependent pathways. Pharmacol Res. 2015 Oct;100:36-46. doi: 10.1016/j.phrs.2015.07.023. Epub 2015 Jul 26. PubMed PMID: 26218603.

15: Møller MN, Kirkeby S, Vikeså J, Nielsen FC, Caye-Thomasen P. Expression of histamine receptors in the human endolymphatic sac: the molecular rationale for betahistine use in Menieres disease. Eur Arch Otorhinolaryngol. 2015 Jul 25. [Epub ahead of print] PubMed PMID: 26208913.

16: Bertlich M, Ihler F, Freytag S, Weiss BG, Strupp M, Canis M. Histaminergic H3-Heteroreceptors as a Potential Mediator of Betahistine-Induced Increase in Cochlear Blood Flow. Audiol Neurootol. 2015;20(5):283-93. doi: 10.1159/000368293. Epub 2015 Jun 27. PubMed PMID: 26139562.

17: Melnikov OA, Lilenko SV, Nauta J, Ouwens MJ. Betahistine plus piracetam dual therapy versus betahistine monotherapy for peripheral vestibular vertigo: a confounder-corrected subanalysis of the OSVaLD study. Curr Med Res Opin. 2015 Nov;31(11):1951-62. doi: 10.1185/03007995.2015.1067193. Epub 2015 Sep 16. PubMed PMID: 26121560.

18: Moorthy G, Sallee F, Gabbita P, Zemlan F, Sallans L, Desai PB. Safety, tolerability and pharmacokinetics of 2-pyridylacetic acid, a major metabolite of betahistine, in a phase 1 dose escalation study in subjects with ADHD. Biopharm Drug Dispos. 2015 Oct;36(7):429-39. doi: 10.1002/bdd.1955. Epub 2015 May 22. PubMed PMID: 25904220.

19: Teggi R, Gatti O, Sykopetrites V, Quaglieri S, Benazzo M, Bussi M. Association of cinnarizine and betahistine in prophylactic therapy for Ménière's disease with and without migraine. Acta Otorhinolaryngol Ital. 2014 Oct;34(5):349-53. Review. PubMed PMID: 25709150; PubMed Central PMCID: PMC4299158.

20: Morozova SV, Alekseeva NS, Lilenko SV, Matsnev EI, Melnikov OA. Effects and safety profile of betahistine in patients in the Russian contingent of OSVaLD, an open-label observational study in vestibular vertigo. Int J Gen Med. 2015 Jan 22;8:47-53. doi: 10.2147/IJGM.S73842. eCollection 2015. PubMed PMID: 25653552; PubMed Central PMCID: PMC4310344.