إيميبتوئين

إيميبتوئين
Systematic (IUPAC) name
	3-(4-chlorophenyl)-5-morpholin-4-yl-4H-imidazol-2-one
Clinical data
Trade names	Pexion
Pregnancy cat.	?
Legal status	?
Routes	Oral
Identifiers
CAS number	188116-07-6
ATCvet code	QN03AX90
PubChem	CID 3083511
ChemSpider	2340703
UNII	19V39682LI
ChEMBL	CHEMBL204240
Synonyms	AWD 131-138; ELB-138
Chemical data
Formula	C13H14ClN3O2
Mol. mass	279.724 g/mol
	InChI InChI=1S/C13H14ClN3O2/c14-10-1-3-11(4-2-10)17-9-12(15-13(17)18)16-5-7-19-8-6-16/h1-4H,5-9H2; Key:IQHYCZKIFIHTAI-UHFFFAOYSA-N;

لم تعد النسخة القابلة للطباعة مدعومة وقد تحتوي على أخطاء في العرض. يرجى تحديث علامات متصفحك المرجعية واستخدام وظيفة الطباعة الافتراضية في متصفحك بدلا منها.

إيميبتوئين Imepitoin (INN) يباع تحت الاسم التجاري بيكسيون Pexion، وهو مضاد اختلاج يستخدم في الطب البيطري في اوروبا لعلاج الصرع عند الكلاب.^[1]^[2]^[3]^[4] لم تتم الموافقة عليه في الولايات المتحدة الأمريكية.^[2]^[3]^[4] يحتوي أيضاً على فعالية مزيلة للقلق.^[1]^[2] طور أساساً لعلاج الصرع عند البشر، لكن تم إنهاءالتجارب السريرية بسبب وجوداختلافات استقلابية غير مرغوب بها عند المدخنين وغير المدخنين.^[1]^[2]

للمركب فعالية كناهض جزئي ذو الفة منخفضة (4,350–5,140 nM منسوب إلى Ki = 6.8 nM للديازيبام وKi = 1.7 nM للكلونازيبام) للموقع البنزوديازبيني لمستقبل ال GABAA (حتى 12-21% من التحفيز الكامل للديازيبام، وناهض تام للموقع).^[1] وهو أول ناهض جزئي يوافق عليه لعلاج الصرع..^[1]

يحجب هذا الدواء بناء على جرعته قنوات الكالسيوم المقيدة بالفولتاج.^[3] هو ليس بنزوديازبين، لكنه عبارة عن إيميدازولون يحمل تشابه هيكلي لمضادات الاختلاج الهدانتوئينية كالإيثوتوئين وفينتوئين.^[1]

مصادر

↑ ^1٫0 ^1٫1 ^1٫2 ^1٫3 ^1٫4 ^1٫5 Rundfeldt C, Löscher W (2014). "The pharmacology of imepitoin: the first partial benzodiazepine receptor agonist developed for the treatment of epilepsy". CNS Drugs. 28 (1): 29–43. PMID 24357084. doi:10.1007/s40263-013-0129-z.
↑ ^2٫0 ^2٫1 ^2٫2 ^2٫3 Sean Sanders (29 April 2015). Seizures in Dogs and Cats. Wiley. pp. 209–. ISBN 978-1-118-68970-7.
↑ ^3٫0 ^3٫1 ^3٫2 Curtis W. Dewey; Ronaldo C. da Costa (8 September 2015). Practical Guide to Canine and Feline Neurology. Wiley. pp. 806–. ISBN 978-1-119-06204-2.
↑ ^4٫0 ^4٫1 https://www.drugs.com/international/imepitoin.html

[pmid24357084-1] 1٫0 ^1٫1 ^1٫2 ^1٫3 ^1٫4 ^1٫5 Rundfeldt C, Löscher W (2014). "The pharmacology of imepitoin: the first partial benzodiazepine receptor agonist developed for the treatment of epilepsy". CNS Drugs. 28 (1): 29–43. PMID 24357084. doi:10.1007/s40263-013-0129-z.

[Sanders2015-2] 2٫0 ^2٫1 ^2٫2 ^2٫3 Sean Sanders (29 April 2015). Seizures in Dogs and Cats. Wiley. pp. 209–. ISBN 978-1-118-68970-7.

[DeweyCosta2015-3] 3٫0 ^3٫1 ^3٫2 Curtis W. Dewey; Ronaldo C. da Costa (8 September 2015). Practical Guide to Canine and Feline Neurology. Wiley. pp. 806–. ISBN 978-1-119-06204-2.

[Drugs.com-4] 4٫0 ^4٫1 https://www.drugs.com/international/imepitoin.html

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v t e GABA_A receptor positive modulators

Alcohols	Brometone Butanol Chloralodol Chlorobutanol (cloretone) Ethanol (alcohol) (alcoholic drink) Ethchlorvynol Isobutanol Isopropanol Menthol Methanol Methylpentynol Pentanol Petrichloral Propanol tert-Butanol (2M2P) tert-Pentanol (2M2B) Tribromoethanol Trichloroethanol Triclofos Trifluoroethanol

Barbiturates	(-)-DMBB Allobarbital Alphenal Amobarbital Aprobarbital Barbexaclone Barbital Benzobarbital Benzylbutylbarbiturate Brallobarbital Brophebarbital Butabarbital/Secbutabarbital Butalbital Buthalital Butobarbital Butallylonal Carbubarb Crotylbarbital Cyclobarbital Cyclopentobarbital Difebarbamate Enallylpropymal Ethallobarbital Eterobarb Febarbamate Heptabarb Heptobarbital Hexethal Hexobarbital Metharbital Methitural Methohexital Methylphenobarbital Narcobarbital Nealbarbital Pentobarbital Phenallymal Phenobarbital Phetharbital Primidone Probarbital Propallylonal Propylbarbital Proxibarbital Reposal Secobarbital Sigmodal Spirobarbital Talbutal Tetrabamate Tetrabarbital Thialbarbital Thiamylal Thiobarbital Thiobutabarbital Thiopental Thiotetrabarbital Valofane Vinbarbital Vinylbital

Benzodiazepines	2-Oxoquazepam 3-Hydroxyphenazepam Adinazolam Alprazolam Arfendazam Avizafone Bentazepam Bretazenil Bromazepam Brotizolam Camazepam Carburazepam Chlordiazepoxide Ciclotizolam Cinazepam Cinolazepam Clazolam Climazolam Clobazam Clonazepam Clonazolam Cloniprazepam Clorazepate Clotiazepam Cloxazolam CP-1414S Cyprazepam Delorazepam Demoxepam Diazepam Diclazepam Doxefazepam Elfazepam Estazolam Ethyl carfluzepate Ethyl dirazepate Ethyl loflazepate Etizolam EVT-201 FG-8205 Fletazepam Flubromazepam Flubromazolam Fludiazepam Flunitrazepam Flunitrazolam Flurazepam Flutazolam Flutemazepam Flutoprazepam Fosazepam Gidazepam Halazepam Haloxazolam Iclazepam Imidazenil Irazepine Ketazolam Lofendazam Lopirazepam Loprazolam Lorazepam Lormetazepam Meclonazepam Medazepam Menitrazepam Metaclazepam Mexazolam Midazolam Motrazepam N-Desalkylflurazepam Nifoxipam Nimetazepam Nitrazepam Nitrazepate Nitrazolam Nordazepam Nortetrazepam Oxazepam Oxazolam Phenazepam Pinazepam Pivoxazepam Prazepam Premazepam Proflazepam Pyrazolam QH-II-66 Quazepam Reclazepam Remimazolam Rilmazafone Ripazepam Ro48-6791 Ro48-8684 SH-053-R-CH3-2′F Sulazepam Temazepam Tetrazepam Tolufazepam Triazolam Triflubazam Triflunordazepam (Ro5-2904) Tuclazepam Uldazepam Zapizolam Zolazepam Zomebazam

Carbamates	Carisbamate Carisoprodol Clocental Cyclarbamate Difebarbamate Emylcamate Ethinamate Febarbamate Felbamate Hexapropymate Lorbamate Mebutamate Meprobamate Nisobamate Pentabamate Phenprobamate Procymate Styramate Tetrabamate Tybamate

Flavonoids	6-Methylapigenin Ampelopsin (dihydromyricetin) Apigenin Baicalein Baicalin Catechin EGC EGCG Hispidulin Linarin Luteolin Rc-OMe Skullcap constituents (e.g., baicalin) Wogonin

Imidazoles	Etomidate Metomidate Propoxate

Kava constituents	10-Methoxyyangonin 11-Methoxyyangonin 11-Hydroxyyangonin Desmethoxyyangonin 11-Methoxy-12-hydroxydehydrokavain 7,8-Dihydroyangonin Kavain 5-Hydroxykavain 5,6-Dihydroyangonin 7,8-Dihydrokavain 5,6,7,8-Tetrahydroyangonin 5,6-Dehydromethysticin Methysticin 7,8-Dihydromethysticin Yangonin

Monoureides	Acecarbromal Apronal (apronalide) Bromisoval Carbromal Capuride Ectylurea

Neuroactive steroids	Acebrochol Allopregnanolone (brexanolone) Alfadolone Alfaxalone 3α-Androstanediol Androstenol Androsterone Certain anabolic-androgenic steroids Cholesterol DHDOC 3α-DHP 5α-DHP 5β-DHP DHT Etiocholanolone Ganaxolone Hydroxydione Minaxolone ORG-20599 ORG-21465 P1-185 Pregnanolone (eltanolone) Progesterone Renanolone SAGE-105 SAGE-217 SAGE-324 SAGE-516 SAGE-689 SAGE-872 Testosterone THDOC

Nonbenzodiazepines	β-Carbolines: Abecarnil Gedocarnil Harmane SL-651,498 ZK-93423 Cyclopyrrolones: Eszopiclone Pagoclone Pazinaclone Suproclone Suriclone Zopiclone Imidazopyridines: Alpidem DS-1 Necopidem Saripidem Zolpidem Pyrazolopyrimidines: Divaplon Fasiplon Indiplon Lorediplon Ocinaplon Panadiplon Taniplon Zaleplon Others: Adipiplon CGS-8216 CGS-9896 CGS-13767 CGS-20625 CL-218,872 CP-615,003 CTP-354 ELB-139 GBLD-345 Imepitoin JM-1232 L-838,417 Lirequinil (Ro41-3696) NS-2664 NS-2710 NS-11394 Pipequaline ROD-188 RWJ-51204 SB-205,384 SX-3228 TGSC01AA TP-003 TPA-023 TP-13 U-89843A U-90042 Viqualine Y-23684

Phenols	Fospropofol Propofol Thymol

Piperidinediones	Glutethimide Methyprylon Piperidione Pyrithyldione

Pyrazolopyridines	Cartazolate Etazolate ICI-190,622 Tracazolate

Quinazolinones	Afloqualone Cloroqualone Diproqualone Etaqualone Mebroqualone Mecloqualone Methaqualone Methylmethaqualone Nitromethaqualone SL-164

Volatiles/gases	Acetone Acetophenone Acetylglycinamide chloral hydrate Aliflurane Benzene Butane Butylene Centalun Chloral Chloral betaine Chloral hydrate Chloroform Cryofluorane Desflurane Dichloralphenazone Dichloromethane Diethyl ether Enflurane Ethyl chloride Ethylene Fluroxene Gasoline Halopropane Halothane Isoflurane Kerosine Methoxyflurane Methoxypropane Nitric oxide Nitrogen Nitrous oxide Norflurane Paraldehyde Propane Propylene Roflurane Sevoflurane Synthane Teflurane Toluene Trichloroethane (methyl chloroform) Trichloroethylene Vinyl ether

Others/unsorted	3-Hydroxybutanal α-EMTBL AA-29504 Avermectins (e.g., ivermectin) Bromide compounds (e.g., lithium bromide, potassium bromide, sodium bromide) Carbamazepine Chloralose Chlormezanone Clomethiazole DEABL Dihydroergolines (e.g., dihydroergocryptine, dihydroergosine, dihydroergotamine, ergoloid (dihydroergotoxine)) DS2 Efavirenz Etazepine Etifoxine Fenamates (e.g., flufenamic acid, mefenamic acid, niflumic acid, tolfenamic acid) Fluoxetine Flupirtine Hopantenic acid Lanthanum Lavender oil Lignans (e.g., 4-O-methylhonokiol, honokiol, magnolol, obovatol) Loreclezole Menthyl isovalerate (validolum) Monastrol Niacin Nicotinamide (niacinamide) Org 25,435 Phenytoin Propanidid Retigabine (ezogabine) Safranal Seproxetine Stiripentol Sulfonylalkanes (e.g., sulfonmethane (sulfonal), tetronal, trional) Terpenoids (e.g., borneol) Topiramate Valerian constituents (e.g., isovaleric acid, isovaleramide, valerenic acid, valerenol) Unsorted benzodiazepine site positive modulators: α-Pinene MRK-409 (MK-0343) TCS-1105 TCS-1205

See also: Receptor/signaling modulators • GABA receptor modulators • GABA metabolism/transport modulators

إيميبتوئين

مصادر

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