Movatterモバイル変換

Adarigiline

From Wikipedia, the free encyclopedia

Pharmaceutical compound

Adarigiline
Clinical data

Drug class	Monoamine oxidase B (MAO-B)inhibitor
Identifiers
IUPAC name (4-hydroxypiperidin-1-yl)-[5-[4-methyl-5-(trifluoromethyl)-1,2-oxazol-3-yl]thiophen-2-yl]methanone
CAS Number	1124197-79-0
PubChemCID	25211190
ChemSpider	64835238
UNII	YRT54V76ZY
Chemical and physical data
Formula	C₁₅H₁₅F₃N₂O₃S
Molar mass	360.35 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES CC1=C(ON=C1C2=CC=C(S2)C(=O)N3CCC(CC3)O)C(F)(F)F
InChI InChI=1S/C15H15F3N2O3S/c1-8-12(19-23-13(8)15(16,17)18)10-2-3-11(24-10)14(22)20-6-4-9(21)5-7-20/h2-3,9,21H,4-7H2,1H3 Key:VXBWTNLAIBIATJ-UHFFFAOYSA-N

Adarigiline (INNTooltip International Nonproprietary Name) is amonoamine oxidase inhibitor (MAOI) that was never marketed.^[1]^[2]^[3]^[4] It is specifically amonoamine oxidase B (MAO-B)inhibitor.^[1]^[2]^[3] This drug candidate was first described in 2009, in apatent assigned to Helicon Therapeutics.^[5]

References

[edit]

^^a ^b"-giline MAO-inhibitors type B C.3.1.0 (a) adarigiline (117),clorgiline (23), mofegiline (69), pargyline (13), rasagiline (70), selegiline (39), sembragiline (111)".Use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances (Stem book 2024)(PDF). World Health Organization. 2024. p. 112.ISBN 978-92-4-009938-8.
^^a ^b"Proposed INN: List 117 International Nonproprietary Names for Pharmaceutical Substances (INN)"(PDF).WHO Drug Information.31 (2). 2017.tadarigilinum adarigiline (4-hydroxypiperidin-1-yl){5-[4-methyl-5-(trifluoromethyl)- 1,2-oxazol-3-yl]thiophen-2-yl}methanone monoamine oxidase B inhibitor [...] C15H15F3N2O3S 1124197-79-0
^^a ^b"Recommended INN: List 79 International Nonproprietary Names for Pharmaceutical Substances (INN)"(PDF).WHO Drug Information.32 (1). 2018.adarigilinum adarigiline (4-hydroxypiperidin-1-yl){5-[4-methyl-5-(trifluoromethyl)- 1,2-oxazol-3-yl]thiophen-2-yl}methanone [...] C15H15F3N2O3S
^"ADARIGILINE".Inxight Drugs. Retrieved24 February 2025.
^WO 2009/029632A1, Kaplan AP, Keenan TP, Mcriner AJ, "Therapeutic isoxazole compounds", published 5 March 2009, assigned to Helicon Therapeutics, Inc.

Monoamine metabolism modulators

Non-specific

AAADTooltip Aromatic L-amino acid decarboxylase

Substrates→Products:L-DOPA (levodopa)→Dopamine
5-HTP→Serotonin
L-Histidine→Histamine
Phenylalanine→Phenethylamine
L-Tyrosine→Tyramine
Tryptophan→Tryptamine

MAOTooltip Monoamine oxidase

Substrates→Products (with ALDHTooltip Aldehyde dehydrogenase/ALRTooltip ALR):Epinephrine (adrenaline)→DHMA Metanephrine→MHPG/VMA Norepinephrine (noradrenaline)→DHMA Normetanephrine→MHPG/VMA Dopamine→DOPAC 3-Methoxytyramine→HVA Serotonin→5-HIAA Inhibitors:Non-selective:Benmoxin Caroxazone Echinopsidine Furazolidone Guineesine Hydralazine Indantadol Iproclozide Iproniazid Isocarboxazid Isoniazid Linezolid Mebanazine Metfendrazine Nialamide Octamoxin Paraxazone Phenelzine Pheniprazine Phenoxypropazine Pivhydrazine Procarbazine Safrazine Tranylcypromine
Inhibitors:MAO-A-selective:Amiflamine Bazinaprine Befloxatone Brofaromine Cimoxatone Clorgiline CX157 (Tyrima) Eprobemide Esuprone Harmala alkaloids (e.g.,harmine,harmaline,harman,norharman,tetrahydroharmine) Methylene blue Metralindole Minaprine Moclobemide Pirlindole Sercloremine Tetrindole Toloxatone
Inhibitors:MAO-B selective:Adarigiline Almoxatone D-Deprenyl Desmethylselegiline Ethanol Ladostigil Lazabemide Milacemide Mofegiline Nicotine Pargyline^‡ Rasagiline Safinamide Selegiline (L-Deprenyl) Sembragiline Tisolagiline Vafidemstat

Phenethylamines
(dopamine,epinephrine,
norepinephrine)

PAHTooltip Phenylalanine hydroxylase	Substrates→Products:Phenylalanine→Tyrosine Inhibitors:3,4-Dihydroxystyrene α-Methylphenylalanine
THTooltip Tyrosine hydroxylase	Substrates→Products:Tyrosine→L-DOPA (levodopa) Inhibitors:2-Hydroxyestradiol 2-Hydroxyestrone 3-Iodotyrosine α-Methyl-5-hydroxytryptophan (α-Me-5-HTP) α-Methylphenylalanine Aquayamycin Bulbocapnine Methyldopa (α-methyl-L-DOPA) Metirosine (α-methyl-p-tyrosine) Oudenone
DBHTooltip Dopamine beta-hydroxylase	Substrates→Products:Dopamine→Norepinephrine (Noradrenaline) Inhibitors:Bupicomide Disulfiram Dopastin Etamicastat Fusaric acid Nepicastat Phenopicolinic acid Tropolone Zamicastat
PNMTTooltip Phenylethanolamine N-methyltransferase	Substrates→Products:Norepinephrine (noradrenaline)→Epinephrine (adrenaline) Inhibitors:CGS-19281A SKF-64139 SKF-7698
COMTTooltip Catechol-O-methyl transferase	Substrates→Products:Dopamine→3-Methoxytyramine DOPAC→Homovanillic acid Norepinephrine→Normetanephrine Epinephrine→Metanephrine DOPEG→MOPEG DOMA→VMA 2-Hydroxyestradiol→2-Methoxyestradiol 2-Hydroxyestrone→2-Methoxyestrone 4-Hydroxyestradiol→4-Methoxyestradiol 4-Hydroxyestrone→4-Methoxyestrone Inhibitors:2-Hydroxyestradiol 2-Hydroxyestrone Entacapone Nebicapone Neluxicapone Nitecapone Opicapone Quinalizarin Tolcapone

Tryptamines
(serotonin,melatonin)

TPHTooltip Tryptophan hydroxylase	Substrates→Products:Tryptophan→5-HTP Inhibitors:AGN-2979 Fenclonine (PCPA) Telotristat ethyl
AANATTooltip Serotonin N-acetyl transferase	Substrates→Products:Serotonin→N-Acetylserotonin
ASMTTooltip Acetylserotonin O-methyltransferase	Substrates→Products:N-Acetylserotonin→Melatonin

Histamine

HDCTooltip Histidine decarboxylase	Substrates→Products:L-Histidine→Histamine Inhibitors:Catechin Alpha-Fluoromethylhistidine Histidine methyl ester Meciadanol Naringenin Tritoqualine
HNMTTooltip Histamine N-methyltransferase	Substrates→Products:Histamine→N-Methylhistamine Inhibitors:Amodiaquine Diphenhydramine Harmaline Metoprine Quinacrine SKF-91488 Tacrine
DAOTooltip Diamine oxidase	Substrates→Products:Histamine→Imidazole acetic acid Inhibitors:Pimagedine (aminoguanidine)

See also:Receptor/signaling modulators •Adrenergics •Dopaminergics •Melatonergics •Serotonergics •Monoamine reuptake inhibitors •Monoamine releasing agents •Monoamine neurotoxins

Thisdrug article relating to thenervous system is astub. You can help Wikipedia byexpanding it.

Retrieved from "https://en.wikipedia.org/w/index.php?title=Adarigiline&oldid=1277397902"

Categories:

Hidden categories:

[8]ページ先頭