Chemistry:5-HT-moduline

From HandWiki

5-Hydroxytryptamine-moduline, also known as 5-HT-moduline or serotonin-moduline as well as Leu-Ser-Ala-Leu (LSAL), is an endogenous neuropeptide and high-affinity serotonin 5-HT1B and 5-HT1D receptor negative allosteric modulator.[1][2][3][4][5][6][7] It is produced in the brain and is co-localized with serotonin 5-HT1B receptor-expressing neurons.[2][8] The compound has been shown to induce desensitization of serotonin 5-HT1B receptors.[2][9] It has been found to increase dopamine release in the striatum in rodents.[10] By inhibiting serotonin 5-HT1B autoreceptors, 5-HT-moduline disinhibits serotonin release and may have antidepressant potential.[1][2] Antibodies and small-molecule antagonists against 5-HT-moduline like HG1 have been found to produce anxiolytic-like effects in rodents.[1][2][11][12][13][14] 5-HT-moduline was first described in the scientific literature by 1996.[2][3] Analogues of 5-HT-moduline have been studied.[15]

References

  1. ↑ 1.0 1.1 1.2 "The role and therapeutic potential of 5-HT-moduline in psychiatry". Seminars in Clinical Neuropsychiatry 8 (2): 137–146. April 2003. doi:10.1053/scnp.2003.50013. PMID 12728412. 
  2. ↑ 2.0 2.1 2.2 2.3 2.4 2.5 "Potential of 5-HT-moduline as a drug target for affective disorders". Current Opinion in Investigational Drugs 1 (1): 104–109. September 2000. PMID 11249585. 
  3. ↑ 3.0 3.1 "A new peptide, 5-HT-moduline, isolated and purified from mammalian brain specifically interacts with 5-HT1B/1D receptors". Behavioural Brain Research 73 (1–2): 313–317. 1996. doi:10.1016/0166-4328(96)00120-9. PMID 8788526. 
  4. ↑ "5-hydroxytryptamine-moduline, a new endogenous cerebral peptide, controls the serotonergic activity via its specific interaction with 5-hydroxytryptamine1B/1D receptors". Molecular Pharmacology 50 (4): 752–762. October 1996. doi:10.1016/S0026-895X(25)09375-7. PMID 8863819. 
  5. ↑ "The endogenous cerebral tetrapeptide 5-HT-moduline reduces in vivo the functional activity of central 5-HT1B receptors in the rat". Neuroscience Research 27 (3): 277–280. March 1997. doi:10.1016/s0168-0102(96)01150-9. PMID 9129186. 
  6. ↑ "Autoradiographic characterization of [3H-5-HT-moduline binding sites in rodent brain and their relationship to 5-HT1B receptors"]. Proceedings of the National Academy of Sciences of the United States of America 94 (18): 9899–9904. September 1997. doi:10.1073/pnas.94.18.9899. PMID 9275223. 
  7. ↑ "Specific interaction of 5-HT-moduline with human 5-HT1b as well as 5-HT1d receptors expressed in transfected cultured cells". Naunyn-Schmiedeberg's Archives of Pharmacology 358 (3): 279–286. September 1998. doi:10.1007/pl00005254. PMID 9774213. 
  8. ↑ "Immunocytochemical localization of neurons expressing 5-HT-moduline in the mouse brain". Neuropharmacology 36 (8): 1079–1087. August 1997. doi:10.1016/s0028-3908(97)00099-3. PMID 9294973. 
  9. ↑ "Molecular, cellular and physiological characteristics of 5-HT-moduline, a novel endogenous modulator of 5-HT1B receptor subtype". Annals of the New York Academy of Sciences 861: 174–182. December 1998. doi:10.1111/j.1749-6632.1998.tb10189.x. PMID 9928255. 
  10. ↑ "5-HT-moduline, a 5-HT(1B/1D) receptor endogenous modulator, interacts with dopamine release measured in vivo by microdialysis". European Journal of Pharmacology 358 (2): 129–137. October 1998. doi:10.1016/s0014-2999(98)00586-x. PMID 9808261. 
  11. ↑ "Drug mechanisms in anxiety". Current Opinion in Investigational Drugs 2 (2): 259–265. February 2001. PMID 11816841. 
  12. ↑ "5-Hydroxytryptamine-moduline: a novel endogenous peptide involved in the control of anxiety". Neuroscience 93 (4): 1223–1225. 1999. doi:10.1016/s0306-4522(99)00322-x. PMID 10501445. 
  13. ↑ "Anxiolytic profile of HG1, a 5-HT-moduline antagonist, in three mouse models of anxiety". European Neuropsychopharmacology 14 (6): 449–456. December 2004. doi:10.1016/j.euroneuro.2003.12.004. PMID 15589384. 
  14. ↑ "Role of GABA-ergic and serotonergic systems in the anxiolytic-like mechanism of action of a 5-HT-moduline antagonist in the mouse elevated plus maze". Behavioural Brain Research 158 (2): 339–348. March 2005. doi:10.1016/j.bbr.2004.09.015. PMID 15698901. 
  15. ↑ "Structural requirements of 5-hydroxytryptamine-moduline analogues to interact with the 5-hydroxytryptamine1B receptor". Journal of Neurochemistry 73 (6): 2617–2620. December 1999. doi:10.1046/j.1471-4159.1999.0732617.x. PMID 10582626. 



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