ASP5736

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ASP5736
Identifiers
  • N-(diaminomethylidene)-1-(2,6-difluorophenyl)-4-fluoroisoquinoline-7-carboxamide
CAS Number
PubChem CID
ChemSpider
ChEMBL
Chemical and physical data
FormulaC17H11F3N4O
Molar mass344.297 g·mol−1
3D model (JSmol)
  • C1=CC(=C(C(=C1)F)C2=NC=C(C3=C2C=C(C=C3)C(=O)N=C(N)N)F)F
  • InChI=1S/C17H11F3N4O/c18-11-2-1-3-12(19)14(11)15-10-6-8(16(25)24-17(21)22)4-5-9(10)13(20)7-23-15/h1-7H,(H4,21,22,24,25)
  • Key:NPYWVXJXMOTDHT-UHFFFAOYSA-N

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

[edit]
  1. ^ Popik P, Krawczyk M, Kuziak A, Bugno R, Hogendorf A, Staroń J, et al. (November 2019). "Serotonin type 5A receptor antagonists inhibit D-lysergic acid diethylamide discriminatory cue in rats". Journal of Psychopharmacology. 33 (11). Oxford, England: 1447–1455. doi:10.1177/0269881119867603. PMID 31452444.
  2. ^ Cyrano E, Popik P (February 2025). "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 : PR. 77 (1): 135–144. doi:10.1007/s43440-024-00679-1. PMC 11743402. PMID 39602080.
  3. ^ Yamazaki M, Harada K, Yamamoto N, Yarimizu J, Okabe M, Shimada T, et al. (October 2014). "ASP5736, a novel 5-HT5A receptor antagonist, ameliorates positive symptoms and cognitive impairment in animal models of schizophrenia". European Neuropsychopharmacology : The Journal of the European College of Neuropsychopharmacology. 24 (10): 1698–1708. doi:10.1016/j.euroneuro.2014.07.009. PMID 25108314.
  4. ^ Yamazaki M, Okabe M, Yamamoto N, Yarimizu J, Harada K (March 2015). "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. doi:10.1016/j.jphs.2015.02.006. PMID 25837935.
  5. ^ Yamazaki M, Yamamoto N, Yarimizu J, Okabe M, Moriyama A, Furutani M, et al. (May 2018). "Functional mechanism of ASP5736, a selective serotonin 5-HT5A receptor antagonist with potential utility for the treatment of cognitive dysfunction in schizophrenia". European Neuropsychopharmacology : The Journal of the European College of Neuropsychopharmacology. 28 (5): 620–629. doi:10.1016/j.euroneuro.2018.03.003. PMID 29571967.
  6. ^ Yamazaki M, Arai T, Yarimizu J, Matsumoto M (September 2022). "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. doi:10.1093/ijnp/pyac041. PMC 9515134. PMID 35882205.
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