Piclozotan

{{Short description|Chemical compound}}

{{Drugbox

| Verifiedfields = changed

| verifiedrevid = 451554695

| IUPAC_name = 3-chloro-4-[4-[4-(2-pyridinyl)-1,2,3,6-tetrahydropyridin-1-yl]butyl]-1,4-benzoxazepin-5(4H)-one

| image = Piclozotan.svg

| tradename =

| pregnancy_category =

| legal_status = Uncontrolled

| routes_of_administration =

| bioavailability =

| metabolism =

| elimination_half-life =

| excretion =

| CAS_number_Ref = {{cascite|correct|??}}

| CAS_number = 182415-09-4

| ATC_prefix =

| ATC_suffix =

| PubChem = 9801640

| ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}}

| UNII_Ref = {{fdacite|correct|FDA}}

| UNII = FQE44HS7AH

| ChemSpiderID = 7977402

| C=23 | H=24 | Cl=1 | N=3 | O=2

| smiles = C1CN(CC=C1C2=CC=CC=N2)CCCCN3C(=COC4=CC=CC=C4C3=O)Cl

| StdInChI_Ref = {{stdinchicite|changed|chemspider}}

| StdInChI = 1S/C23H24ClN3O2/c24-22-17-29-21-9-2-1-7-19(21)23(28)27(22)14-6-5-13-26-15-10-18(11-16-26)20-8-3-4-12-25-20/h1-4,7-10,12,17H,5-6,11,13-16H2

| StdInChIKey_Ref = {{stdinchicite|changed|chemspider}}

| StdInChIKey = URMTUEWUIGOJBW-UHFFFAOYSA-N

}}

Piclozotan (SUN-N4057) is a selective 5-HT1A receptor partial agonist, which has neuroprotective effects in animal studies.{{cite journal | vauthors = Kamei K, Maeda N, Nomura K, Shibata M, Katsuragi-Ogino R, Koyama M, Nakajima M, Inoue T, Ohno T, Tatsuoka T | display-authors = 6 | title = Synthesis, SAR studies, and evaluation of 1,4-benzoxazepine derivatives as selective 5-HT1A receptor agonists with neuroprotective effect: Discovery of Piclozotan | journal = Bioorganic & Medicinal Chemistry | volume = 14 | issue = 6 | pages = 1978–92 | date = March 2006 | pmid = 16290165 | doi = 10.1016/j.bmc.2005.10.046 }} It has been through early clinical trials in humans for treatment of acute stroke, but results have not yet been announced.{{cite journal | vauthors = Ferro JM, Dávalos A | title = Other neuroprotective therapies on trial in acute stroke | journal = Cerebrovascular Diseases | volume = 21 Suppl 2 | issue = 2 | pages = 127–30 | year = 2006 | pmid = 16651823 | doi = 10.1159/000091712 | s2cid = 39193793 }}{{cite journal | vauthors = Mondick JT, Oo C, Patel D, Fujitani T, Shimizu K, Barrett JS | title = Population pharmacokinetics of the selective serotonin 5-HT1A receptor partial agonist piclozotan | journal = American Journal of Therapeutics | volume = 16 | issue = 2 | pages = 106–15 | year = 2009 | pmid = 19300037 | doi = 10.1097/MJT.0b013e31816b8c85 | s2cid = 21284395 }}

See also

References