ASP5736

{{cs1 config|name-list-style=vanc|display-authors=6}}

{{Infobox drug

| IUPAC_name = N-(diaminomethylidene)-1-(2,6-difluorophenyl)-4-fluoroisoquinoline-7-carboxamide

| image = ASP5736.svg

| width = 240

| tradename =

| legal_status =

| routes_of_administration =

| metabolism =

| elimination_half-life =

| excretion =

| CAS_number = 1264206-74-7

| UNII =

| PubChem = 50923443

| ChemSpiderID = 58951462

| ChEMBL = 3644528

| C=17 | H=11 | F=3 | N=4 | O=1

| smiles = C1=CC(=C(C(=C1)F)C2=NC=C(C3=C2C=C(C=C3)C(=O)N=C(N)N)F)F

| StdInChI = 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)

| StdInChIKey = 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,{{cite journal | vauthors = Popik P, Krawczyk M, Kuziak A, Bugno R, Hogendorf A, Staroń J, Nikiforuk A | title = Serotonin type 5A receptor antagonists inhibit D-lysergic acid diethylamide discriminatory cue in rats | journal = Journal of Psychopharmacology | volume = 33 | issue = 11 | pages = 1447–1455 | date = November 2019 | pmid = 31452444 | doi = 10.1177/0269881119867603 }}{{cite journal | vauthors = Cyrano E, Popik P | title = 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 | journal = Pharmacological Reports | volume = 77 | issue = 1 | pages = 135–144 | date = February 2025 | pmid = 39602080 | pmc = 11743402 | doi = 10.1007/s43440-024-00679-1 }} 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.{{cite journal | vauthors = Yamazaki M, Harada K, Yamamoto N, Yarimizu J, Okabe M, Shimada T, Ni K, Matsuoka N | title = ASP5736, a novel 5-HT5A receptor antagonist, ameliorates positive symptoms and cognitive impairment in animal models of schizophrenia | journal = European Neuropsychopharmacology | volume = 24 | issue = 10 | pages = 1698–1708 | date = October 2014 | pmid = 25108314 | doi = 10.1016/j.euroneuro.2014.07.009 | doi-access = free }}{{cite journal | vauthors = Yamazaki M, Okabe M, Yamamoto N, Yarimizu J, Harada K | title = Novel 5-HT5A receptor antagonists ameliorate scopolamine-induced working memory deficit in mice and reference memory impairment in aged rats | journal = Journal of Pharmacological Sciences | volume = 127 | issue = 3 | pages = 362–369 | date = March 2015 | pmid = 25837935 | doi = 10.1016/j.jphs.2015.02.006 | doi-access = free }}{{cite journal | vauthors = Yamazaki M, Yamamoto N, Yarimizu J, Okabe M, Moriyama A, Furutani M, Marcus MM, Svensson TH, Harada K | title = Functional mechanism of ASP5736, a selective serotonin 5-HT5A receptor antagonist with potential utility for the treatment of cognitive dysfunction in schizophrenia | journal = European Neuropsychopharmacology | volume = 28 | issue = 5 | pages = 620–629 | date = May 2018 | pmid = 29571967 | doi = 10.1016/j.euroneuro.2018.03.003 | doi-access = free }}{{cite journal | vauthors = Yamazaki M, Arai T, Yarimizu J, Matsumoto M | title = 5-HT5A Receptor Antagonist ASP5736 Ameliorates Several Abnormal Behaviors in an Fmr1-Targeted Transgenic Male Rat Model of Fragile X Syndrome | journal = The International Journal of Neuropsychopharmacology | volume = 25 | issue = 9 | pages = 786–793 | date = September 2022 | pmid = 35882205 | pmc = 9515134 | doi = 10.1093/ijnp/pyac041 }}

References