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. Author manuscript; available in PMC: 2014 Jul 8.
Published in final edited form as: Curr Top Med Chem. 2013;13(11):1353–1362. doi: 10.2174/15680266113139990039

Table 2.

List of some human 5-HT2B receptor agonists and antagonists and their therapeutic indications.

5-HT2B Agents Name Structure Mechanism of action Therapeutic Indication
Fenfluramine22 graphic file with name nihms-607291-t0006.jpg Increases Serotonin levels Controls food intake or suppresses Obesity
Norfenfluramine22 graphic file with name nihms-607291-t0007.jpg Metabolite of Fenfluramine. Increases Serotonin levels Controls food intake or suppresses Obesity
3,4-methylenedioxymeth amphetamine (MDMA, “Ecstasy”)25 graphic file with name nihms-607291-t0008.jpg Increases Serotonin levels Posttraumatic stress disorder, Psychotherapy
Alpha-methyl-5 -HT33 graphic file with name nihms-607291-t0009.jpg Increases Serotonin levels Its prodrug alpha- methyltryptophan is used for treatment of disorders where serotonin is deficient
AGONISTS Lysergic acid diethylamide (LSD)3 graphic file with name nihms-607291-t0010.jpg 5-HT receptor agonist Psychotherapy, Pain, Alcoholism etc.
Carbergoline42 graphic file with name nihms-607291-t0011.jpg Dopamine agonist hyperprolactinemia, Parkinson's disease etc.
Dihydroergotamine42 graphic file with name nihms-607291-t0012.jpg Serotonin receptor agonist Migraine treatment
Methylergonovine42 graphic file with name nihms-607291-t0013.jpg Partial agonist/antagoni st on serotonergic, dopaminergic and alpha- adrenergic receptors Control of postpartum hemorrhage & Migraines
Pergolide42 graphic file with name nihms-607291-t0014.jpg Dopamine agonist Parkinson’s Disease and Hyperprolactinemic Disorders
Agomelatine3 graphic file with name nihms-607291-t0015.jpg MTi and MT2 agonist as well as 5-HT2C antagonist Antidepressant
ANTAGONI STS Asenapine3 graphic file with name nihms-607291-t0016.jpg Schizophrenia and mania associated with bipolar disorder
Ketanserin3 graphic file with name nihms-607291-t0017.jpg alpha-1 adrenergic receptor antagonist Antihypertensive
Methysergide3 graphic file with name nihms-607291-t0018.jpg 5-HT2B receptor agonist Treatment of Migraines
Ritanserin3 graphic file with name nihms-607291-t0019.jpg 5HT2A/2C antagonist Treatment of schizophrenia
Tegaserod3 graphic file with name nihms-607291-t0020.jpg 5-HT4 agonist Management of irritable bowel syndrome and constipation
Yohimbine3 graphic file with name nihms-607291-t0021.jpg Alpha-2 andrenergic receptor antagonist Treatment of impotence or erectile dysfunction