Chemistry:ASP5736

From HandWiki

ASP5736 is an experimental drug developed by Astellas Pharma, which acts as a selective antagonist for the serotonin receptor 5-HT5A, with significantly higher potency than the older drug SB-699,551. In animal studies, it was found to reduce drug appropriate responding produced by LSD, but not DOI,[1][2] and has also been found to reduce the cognitive dysfunction and memory deficits produced by scopolamine in animal studies, which has been suggested may indicate a potential role for 5-HT5A antagonists in the treatment of schizophrenia, as well as other conditions such as fragile X syndrome.[3][4][5][6]

References

  1. ↑ "Serotonin type 5A receptor antagonists inhibit D-lysergic acid diethylamide discriminatory cue in rats". Journal of Psychopharmacology 33 (11): 1447–1455. November 2019. doi:10.1177/0269881119867603. PMID 31452444. 
  2. ↑ "Assessing the effects of 5-HT2A and 5-HT5A receptor antagonists on DOI-induced head-twitch response in male rats using marker-less deep learning algorithms". Pharmacological Reports 77 (1): 135–144. February 2025. doi:10.1007/s43440-024-00679-1. PMID 39602080. 
  3. ↑ "ASP5736, a novel 5-HT5A receptor antagonist, ameliorates positive symptoms and cognitive impairment in animal models of schizophrenia". European Neuropsychopharmacology 24 (10): 1698–1708. October 2014. doi:10.1016/j.euroneuro.2014.07.009. PMID 25108314. 
  4. ↑ "Novel 5-HT5A receptor antagonists ameliorate scopolamine-induced working memory deficit in mice and reference memory impairment in aged rats". Journal of Pharmacological Sciences 127 (3): 362–369. March 2015. doi:10.1016/j.jphs.2015.02.006. PMID 25837935. 
  5. ↑ "Functional mechanism of ASP5736, a selective serotonin 5-HT5A receptor antagonist with potential utility for the treatment of cognitive dysfunction in schizophrenia". European Neuropsychopharmacology 28 (5): 620–629. May 2018. doi:10.1016/j.euroneuro.2018.03.003. PMID 29571967. 
  6. ↑ "5-HT5A Receptor Antagonist ASP5736 Ameliorates Several Abnormal Behaviors in an Fmr1-Targeted Transgenic Male Rat Model of Fragile X Syndrome". The International Journal of Neuropsychopharmacology 25 (9): 786–793. September 2022. doi:10.1093/ijnp/pyac041. PMID 35882205. 



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