betahistine mesilate
Betahistine is an orally administered, centrally acting histamine H1 receptor agonist with partial H3 antagonistic activity. It is proposed that betahistine may reduce peripherally the asymmetric functioning of the sensory vestibular organs in addition to increasing vestibulocochlear blood flow by antagonising local H3 heteroreceptors. Betahistine acts centrally by enhancing histamine synthesis within tuberomammillary nuclei of the posterior hypothalamus and histamine release within vestibular nuclei through antagonism of H3 autoreceptors. This mechanism, together with less specific effects of betahistine on alertness regulation through cerebral H1 receptors, should promote and facilitate central vestibular compensation. Betahistine is used to treat the symptoms associated with Ménière's disease, a condition of the inner ear which causes, vertigo (dizziness), tinnitus (ringing in the ears), hearing loss. — NCATS
Clinical trial activity
37 trials · 54 clinical orgs · 0 marketing orgs
Earliest trial started Jan 1, 2003 (NCT00160238)
Timeline
Indications
Approved for
Studied for
- Affective Disorders, Psychotic · Phase 2
- Anemia · Phase 4
- Attention Deficit Disorder with Hyperactivity · Phase 1
- Autism Spectrum Disorder · Phase 2
- Bipolar Disorder · Phase 2
- Depression · Phase 2
- Dyslipidemias · Phase 3
- Healthy Volunteers · Phase 1
- Hypercholesterolemia · Phase 2
- Hypophosphatemia · Phase 4
- Iron Deficiencies · Phase 4
- Meniere Disease · Phase 4
- Obesity · Phase 3
- Overnutrition · Phase 1
- Overweight · Phase 1
- Postural Balance · Phase 4
- Psychotic Disorders · Phase 2
- Schizophrenia · Phase 2
- Vertigo · Phase 4
- Weight Gain · Phase 2
Mechanism of action
- Histamine H1 receptorAGONIST
HRH1 agonist
Betahistine has a very strong affinity as an antagonist for histamine H3 receptors and a weak affinity as an agonist for histamine H1 receptors. Its efficacy can be explained by mechanisms targeting these histamine receptors (HRs) at three different levels: the vascular tree, with an increase of cochlear and vestibular blood flow involving the H1R; the central nervous system, with an increase of histamine turnover implicating the H3R, and the peripheral labyrinth, with a decrease of vestibular input implying the H3R/H4R.
Betahistine is a strong Histamine H3 receptor antagonist and a weak Histamine H1 agonist.
- Histamine receptor H3ANTAGONIST
HRH3 antagonist
- Histamine H3 receptorANTAGONIST
HRH3 antagonist
Betahistine has a very strong affinity as an antagonist for histamine H3 receptors and a weak affinity as an agonist for histamine H1 receptors. Its efficacy can be explained by mechanisms targeting these histamine receptors (HRs) at three different levels: the vascular tree, with an increase of cochlear and vestibular blood flow involving the H1R; the central nervous system, with an increase of histamine turnover implicating the H3R, and the peripheral labyrinth, with a decrease of vestibular input implying the H3R/H4R.
Betahistine is a strong Histamine H3 receptor antagonist and a weak Histamine H1 agonist.
Chemistry & pharmacology
SMILES
CNCCc1ccccn1- Mol. weight
- 136.2 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- Yes
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL24441 ↗
- WikipediaTee (symbol) ↗
- NCATSX32KK4201D ↗
- ChEMBLCHEMBL1446813 ↗
- WikipediaBetahistine ↗
Also known as
- 2-[2-(methylamino)ethyl]pyridine
- 2-[2-(methylamino)ethyl]pyridine
- [2-(2-pyridyl)ethyl]methylamine
- [2-(2-pyridyl)ethyl]methylamine
- 2-(beta-methylaminoethyl)pyridine
- 2-(beta-methylaminoethyl)pyridine
- betahistina
- betahistina
- betahistine
- betahistine
- betahistine
- betahistine
- betahistine
- betahistine
- betahistine
- beta-histine
- betahistine dihydrobromide
- betahistine dihydrochloride
- betahistine dihydrochloride
- betahistine dihydrochloride
- betahistine dihydrochloride
- betahistine dihydrochloride
- betahistine dihydrochloride
- betahistine dihydrochloride
- betahistine hcl
- betahistine hcl
- betahistine hydrochloride
- betahistine hydrochloride
- betahistine hydrochloride
- betahistine hydrochloride
- betahistine mesilate
- betahistine mesilate
- betahistine mesilate
- betahistine mesilate
- betahistine mesylate
- betahistine methanesulfonate
- betahistinum
- betahistinum
- merislon
- n-methyl-2-(2-pyridinyl)ethanamine
- n-methyl-2-(2-pyridinyl)ethanamine
- n-methyl-2-pyridineethanamine
- n-methyl-2-pyridineethanamine
- pt-9
- pt-9
- serc
- serc
- serc-16
- serc-8
- verum
- verum
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT07017244 | N/A | Jun 15, 2025 | Azienda Ospedaliera Universitaria Policlinico G. Martino |
| NCT07075289 | Phase 4 | Apr 1, 2024 | Dexa Medica Group, Universitas Sebelas Maret |
| NCT06001593 | Phase 1/Phase 2 (Phase 2) | Sep 7, 2023 | Seoul National University |
| NCT06123234 | N/A | Apr 1, 2023 | Azienda Ospedaliera Universitaria Policlinico G. Martino |
| NCT05757050 | N/A | Mar 13, 2023 | A. Vogel AG, Newcastle University |
| NCT05604937 | N/A | Dec 31, 2022 | Shanghai University of Traditional Chinese Medicine |
| NCT05598749 | N/A | Oct 31, 2022 | Fytexia, Universidad Católica San Antonio de Murcia |
| NCT06218225 | N/A | Oct 15, 2022 | Azienda Ospedaliera Universitaria Policlinico G. Martino |
| NCT05472285 | N/A | May 23, 2022 | Biofortis, Bionov |
| NCT05098249 | Phase 4 | Nov 11, 2021 | University of Zurich |
| NCT05938517 | Phase 1 | Jun 2, 2021 | Ludwig Maximilians University |
| NCT06544434 | Phase 2 | May 1, 2021 | Capital Medical University |
| NCT05328895 | N/A | Oct 1, 2020 | Capital Medical University |
| NCT03823196 | N/A | Mar 8, 2019 | Fytexia, Universidad Católica San Antonio de Murcia |
| NCT03624283 | N/A | Sep 1, 2018 | Fudan University |
| NCT03627117 | N/A | Aug 13, 2018 | University of Basel |
| NCT07059533 | N/A | Mar 31, 2017 | Ecole Polytechnique Fédérale de Lausanne |
| NCT04283266 | N/A | Jun 12, 2016 | Vesale Pharma |
| NCT02392767 | N/A | Oct 1, 2014 | BioTeSys GmbH, Dr. Loges & Co. GmbH |
| NCT02026778 | N/A | Dec 1, 2013 | Yonsei University |
Organizations
Research & Development (54)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| OBEcure Ltd. | For profit | 6 | 6 | 2 | 2007 |
| Azienda Ospedaliera Universitaria Policlinico G. Martino | Academic/Hospital | 3 | 3 | 1 | 2022 |
| Capital Medical University | Academic/Hospital | 3 | 2 | 3 | 2007 |
| Fytexia | Academic/Hospital | 2 | 2 | 1 | 2019 |
| Universidad Católica San Antonio de Murcia | Academic/Hospital | 2 | 0 | 1 | 2019 |
| University of Cincinnati | Academic/Hospital | 2 | 1 | 1 | 2006 |
| Abbott | For profit | 1 | 1 | 1 | 2012 |
| Alvogen | For profit | 1 | 1 | 1 | 2013 |
| A. Vogel AG | For profit | 1 | 1 | 1 | 2023 |
| Biofortis | For profit | 1 | 0 | 1 | 2022 |
| Bionov | For profit | 1 | 1 | 1 | 2022 |
| BioTeSys GmbH | For profit | 1 | 0 | 1 | 2014 |
| Bonn Education Association for Dietetics r.A., Cologne, Germany | Academic/Hospital | 1 | 1 | 1 | 2004 |
| Cahaba Research, Inc | For profit | 1 | 0 | 1 | 2007 |
| Covance | For profit | 1 | 0 | 1 | 2007 |
| Dexa Medica Group | For profit | 1 | 0 | 1 | 2024 |
| Diablo Clinical Research | For profit | 1 | 0 | 1 | 2007 |
| Dr. Loges & Co. GmbH | For profit | 1 | 1 | 1 | 2014 |
| Ecole Polytechnique Fédérale de Lausanne | Academic/Hospital | 1 | 1 | 1 | 2017 |
| Eisai | For profit | 1 | 1 | 1 | 2007 |