Tiomergine (INNTooltip International Nonproprietary Name; developmental code name CF 25-397) is a dopamine receptor agonist of the ergoline family which was never marketed.[1][2][3][4] It is an analogue of the antiparkinsonian agent pergolide.[1][2]

In addition to its dopamine receptor agonism, tiomergine also acts as a potent serotonin receptor agonist, including binding to serotonin 5-HT1 and 5-HT2 receptors, and might actually act primarily via its serotonin receptor agonism.[5][6][7][8] The drug produces antiparkinsonian-like effects in rodents.[9] In contrast to other dopamine receptor agonists however, it produces little to no stereotypy.[9] In addition, tiomergine produces little change in locomotor activity on its own but reverses reserpine-induced catalepsy.[9] Unlike many other dopamine receptor agonists like pergolide, tiomergine has been identified as a selective or preferential dopamine autoreceptor agonist, with little activity at postsynaptic receptors.[10][11][12]

In contrast to animal studies, tiomergine caused severe deterioration in parkinsonism symptoms in humans in a clinical trial.[13][14] It was also ineffective in treating psychosis in people with schizophrenia.[15] Besides these uses, tiomergine has been investigated for the treatment of dyskinesia and dystonia.[16][17] However, it was ineffective for tardive dyskinesia as well.[17]

Tiomergine was first described in the scientific literature by 1976.[9] It was developed by Sandoz.[3]

See also

References

  1. 1 2 Elks J (14 November 2014). The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. ISBN 978-1-4757-2085-3. Retrieved 5 May 2026.
  2. 1 2 Ganellin CR, Triggle DJ (21 November 1996). Dictionary of Pharmacological Agents. CRC Press. ISBN 978-0-412-46630-4. Retrieved 5 May 2026.
  3. 1 2 Hansch C, Sammes PG, Taylor JB (1990). Comprehensive Medicinal Chemistry: The Rational Design, Mechanistic Study & Therapeutic Applications of Chemical Compounds. Pergamon Press. ISBN 978-0-08-032530-9. Retrieved 5 May 2026.
  4. ↑ Negwer M (2001). Organic-chemical Drugs and Their Synonyms: An International Survey. Wiley-VCH. ISBN 978-3-527-30247-5. Retrieved 5 May 2026.
  5. ↑ Markstein R, Hoyer D, Engel G (August 1986). "5-HT1A-receptors mediate stimulation of adenylate cyclase in rat hippocampus". Naunyn-Schmiedeberg's Archives of Pharmacology. 333 (4): 335–341. doi:10.1007/BF00500006. PMID 2945992.
  6. ↑ Vigouret JM, Bürki HR, Jaton AL, Züger PE, Loew DM (1978). "Neurochemical and neuropharmacological investigations with four ergot derivatives: bromocriptine, dihydroergotoxine, CF 25-397 and CM 29-712". Pharmacology. 16 Suppl 1: 156–173. doi:10.1159/000136817. PMID 565520.
  7. ↑ Loew DM, Vigouret JM, Jaton AL (1979). "Neuropharmacology of Ergot Derivatives". Dopaminergic Ergot Derivatives and Motor Function. Elsevier. pp. 129–140. doi:10.1016/b978-0-08-024408-2.50015-4. ISBN 978-0-08-024408-2.
  8. ↑ Bürki HR, Asper H, Ruch W, Züger PE (May 1978). "Bromocriptine, dihydroergotoxine, methysergide, d-LSD, CF25--397, and 29--712: effects on the metabolism of the biogenic amines in the brain of the rat". Psychopharmacology. 57 (3): 227–237. doi:10.1007/BF00426743. PMID 97702.
  9. 1 2 3 4 Jaton AL, Loew DM, Vigouret JM (March 1976). "Proceedings: CF 25-397 (9, 10-didehydro-6-methyl-8beta-(2-pyridylthiomethyl) ergoline), a new central dopamine receptor agonist". British Journal of Pharmacology. 56 (3): 371P. PMC 1666968. PMID 944059.
  10. ↑ Fuxe K, Fredholm BB, Agnati LF, Ogren SO, Everitt BJ, Jonsson G, et al. (1978). "Interaction of ergot drugs with central monoamine systems. Evidence for a high potential in the treatment of mental and neurological disorders". Pharmacology. 16 Suppl 1: 99–134. doi:10.1159/000136813. PMID 643908.
  11. ↑ Martin GE, Bendesky RJ (June 1984). "Mouse locomotor activity: an in vivo test for dopamine autoreceptor activation". The Journal of Pharmacology and Experimental Therapeutics. 229 (3): 706–711. doi:10.1016/S0022-3565(25)21892-4. PMID 6144790.
  12. ↑ Palacios JM, Wiederhold KH (September 1984). "Presynaptic dopaminergic agonists modify brain glucose metabolism in a way similar to the neuroleptics". Neuroscience Letters. 50 (1–3): 223–229. doi:10.1016/0304-3940(84)90490-7. PMID 6149502.
  13. ↑ Calne DB, Williams AC, Nutt JG, Neophytides A, Eisler T, Teychenne PF (November 1978). "Ergot derivatives for Parkinsonism". The Medical Journal of Australia. 2 (3 Suppl): 25–26. doi:10.5694/j.1326-5377.1978.tb77384.x. PMID 34083.
  14. ↑ Teychenne PF, Pfeiffer R, Bern SM, Calne DB (December 1977). "Experiences with a new ergoline (CF 25-397) in parkinsonism". Neurology. 27 (12): 1140–1143. doi:10.1212/wnl.27.12.1140. PMID 563012.
  15. ↑ Tamminga CA, Schaffer MH (1979). "Treatment of Schizophrenia with ergot derivatives". Psychopharmacology. 66 (3): 239–242. doi:10.1007/BF00428312. PMID 119270.
  16. ↑ Frattola L, Albizzati MG, Bassi S, Spano PF, Trabucchi M (1980). "Treatment of dyskinetic and dystonic disorders with CF 25-397: clinical and pharmacological aspects". Advances in Biochemical Psychopharmacology. 23: 381–386. PMID 6446848.
  17. 1 2 Tamminga CA, Chase TN (April 1980). "Bromocriptine and CF 25-397 in the treatment of tardive dyskinesia". Archives of Neurology. 37 (4): 204–205. doi:10.1001/archneur.1980.00500530042004. PMID 6102461.
source: https://en.wikipedia.org/wiki/Tiomergine