Serotonin agonist
Serotonin agonists , also known as serotonin receptor agonists , are pharmacologically active substances that, like tissue hormone and neurotransmitter serotonin , can activate serotonin receptors . These agonists can be distinguished on the basis of their selectivity for at least 14 different serotonin receptors. Serotonin agonists are used, for example, in the treatment of anxiety disorders and migraines . Other representatives, however, have a meaning as psychedelically effective intoxicating drugs .
selection
Serotonin agonist | selectivity | use |
---|---|---|
Serotonin | 5-HT 1 to 5-HT 7 | endogenous ligand |
5-carboxamidotryptamine | 5-HT 1 , 5-HT 5 , 5-HT 7 | - |
Azapirones (e.g. buspirone , tandospirone ) |
5-HT 1A | Treating anxiety disorders |
Methylphenidate | 5-HT 1A & 5-HT 2b | Treatment of AD (H) S |
Triptans (e.g. sumatriptan , almotriptan , eletriptan , naratriptan , rizatriptan , zolmitriptan ) |
5-HT 1B , 5-HT 1D | Migraine therapy |
Various hallucinogenic amphetamines : 2,5-dimethoxy-4-bromamphetamine (DOB), 2,5-dimethoxy-4-iodamphetamine (DOI) | 5-HT 2A / 2B / 2C | Psychedelic, serotonin receptor research chemical |
Various other hallucinogenic phenylethylamines , e.g. B. Mescaline , 4-bromo-2,5-dimethoxyphenylethylamine (2C-B), 2,5-dimethoxy-4-ethylphenylethylamine (2C-E), 25I-NBOMe ( full agonist ) | 5-HT 2A / 2C | Psychedelic |
Various hallucinogenic tryptamines and related indole alkaloids , e.g. B. Lysergic acid diethylamide (LSD), psilocybin , ergin (LSA) | 5-HT 2A / 2C | Psychedelic |
Dimethyltryptamine (DMT, full agonist) | 5-HT 2A / 2C | Psychedelic, presumably an endogenous ligand at the σ1 receptor |
Lorcaserin | 5-HT 2C | Appetite suppressants |
Cisapride | 5-HT 4 | Prokinetic |
Tegaserod | 5-HT 4 | Irritable bowel syndrome |
literature
- Hoyer D, Clarke DE, Fozard JR, et al. : International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (serotonin) . In: Pharmacol. Rev. . 46, No. 2, June 1994, pp. 157-203. PMID 7938165 .
- Hoyer D, Hannon JP, Martin GR: Molecular, pharmacological and functional diversity of 5-HT receptors . In: Pharmacol. Biochem. Behav. . 71, No. 4, April 2002, pp. 533-554. PMID 11888546 .
Individual evidence
- ↑ RHP Porter, KR Benwell, H. Lamb, CS Malcolm, NH Allen, DF Revell, DR Adams, MJ Sheardown: Functional characterization of agonists at recombinant human 5-HT, 5-HT and 5-HT receptors in CHO-K1 cells . In: British Journal of Pharmacology. 128, 1999, pp. 13-20, doi : 10.1038 / sj.bjp.0702751 .
- ^ Thomas S. Ray, Olivier Jacques Manzoni: Psychedelics and the Human Receptorome. In: PLoS ONE. 5, 2010, p. E9019, doi : 10.1371 / journal.pone.0009019 .
- ↑ Fontanilla D., Johannessen M., Hajipour AR, Cozzi NV, Jackson MB, Ruoho AE: The Hallucinogen N, N-Dimethyltryptamine (DMT) Is an Endogenous Sigma-1 Receptor Regulator . In: Science . 323, No. 5916, February 2009, pp. 934-7. doi : 10.1126 / science.1166127 . PMID 19213917 . PMC 2947205 (free full text).
- ↑ Su TP, Hayashi T., Vaupel DB: When the Endogenous Hallucinogenic Trace Amine N, N-Dimethyltryptamine Meets the Sigma-1 Receptor . In: Science Signaling . 2, No. 61, 2009, p. Pe12. doi : 10.1126 / scisignal.261pe12 . PMID 19278957 . PMC 3155724 (free full text).