Tìm theo
Aprobarbital
Các tên gọi khác (7 ) :
  • 5-(1-Methylethyl)-5-(2-propenyl)-2,4,6(1H,3H,5H)-pyrimidinetrione
  • 5-Allyl-5-isopropylbarbituric acid
  • 5-Allyl-5-isopropylpyrimidine-2,4,6(1H,3H,5H)-trione
  • 5-Isopropyl-5-allylbarbituric acid
  • Allypropymal
  • Alurate
  • Aprobarbital
Thuốc Gốc
Small Molecule
CAS: 77-02-1
ATC: N05CA05
CTHH: C10H14N2O3
PTK: 210.2298
Aprobarbital is a barbiturate derivative synthesized in the 1920s by Ernst Preiswerk. It has sedative, hypnotic and anticonvulsant properties, and was used primarily for the treatment of insomnia. Aprobarbital was never as widely used as more common barbiturate derivatives such as phenobarbital and is now rarely prescribed.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
Phân tử khối
210.2298
Monoisotopic mass
210.100442324
InChI
InChI=1S/C10H14N2O3/c1-4-5-10(6(2)3)7(13)11-9(15)12-8(10)14/h4,6H,1,5H2,2-3H3,(H2,11,12,13,14,15)
InChI Key
InChIKey=UORJNBVJVRLXMQ-UHFFFAOYSA-N
IUPAC Name
5-(prop-2-en-1-yl)-5-(propan-2-yl)-1,3-diazinane-2,4,6-trione
Traditional IUPAC Name
aprobarbital
SMILES
CC(C)C1(CC=C)C(=O)NC(=O)NC1=O
Độ tan chảy
141 °C
Độ hòa tan
4080 mg/L (at 25 °C)
logP
1.15
logS
-1.6
pKa (strongest acidic)
8.48
PSA
75.27 Å2
Refractivity
53.45 m3·mol-1
Polarizability
20.5 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
3
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
1
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
7.99 (at 25 °C)
Cơ Chế Tác Dụng : Aprobarbital is a barbiturate derivative synthesized in the 1920s by Ernst Preiswerk. It has sedative, hypnotic and anticonvulsant properties, and was used primarily for the treatment of insomnia. Aprobarbital was never as widely used as more common barbiturate derivatives such as phenobarbital and is now rarely prescribed. Aprobarbital (like all barbiturates) works by binding to the GABAA receptor at either the alpha or the beta sub unit. These are binding sites that are distinct from GABA itself and also distinct from the benzodiazepine binding site. Like benzodiazepines, barbiturates potentiate the effect of GABA at this receptor. This GABAA receptor binding decreases input resistance, depresses burst and tonic firing, especially in ventrobasal and intralaminar neurons, while at the same time increasing burst duration and mean conductance at individual chloride channels; this increases both the amplitude and decay time of inhibitory postsynaptic currents. In addition to this GABA-ergic effect, barbiturates also block the AMPA receptor, a subtype of glutamate receptor. Glutamate is the principal excitatory neurotransmitter in the mammalian CNS. Aprobarbital also appears to bind neuronal nicotinic acetylcholine receptors.
Tương Tác Thuốc :
  • Aminophylline The barbiturate, aprobarbital, decreases the effect of aminophylline.
  • Betamethasone The barbiturate, aprobarbital, may decrease the effect of the corticosteroid, betamethasone.
  • Clomifene The enzyme inducer, aprobarbital, decreases the effect of the hormone agent, clomifene.
  • Conjugated Estrogens The enzyme inducer, aprobarbital, decreases the effect of the hormone agent, conjugated estrogens.
  • Cyclosporine The barbiturate, aprobarbital, increases the effect of cyclosporine.
  • Dexamethasone The barbiturate, aprobarbital, may decrease the effect of the corticosteroid, dexamethasone.
  • Diethylstilbestrol The enzyme inducer, aprobarbital, decreases the effect of the hormone agent, diethylstilbestrol.
  • Doxycycline The anticonvulsant, aprobarbital, decreases the effect of doxycycline.
  • Estradiol The enzyme inducer, aprobarbital, decreases the effect of the hormone agent, estradiol.
  • Ethinyl Estradiol This product may cause a slight decrease of contraceptive effect
  • Felodipine The barbiturate, aprobarbital, decreases the effect of felodipine.
  • Fludrocortisone The barbiturate, aprobarbital, may decrease the effect of the corticosteroid, fludrocortisone.
  • Folic Acid Folic acid decreases the effect of anticonvulsant, aprobarbital.
  • Gefitinib The CYP3A4 inducer, aprobarbital, may decrease the serum concentration and therapeutic effects of gefitinib.
  • Griseofulvin The barbiturate, aprobarbital, decreases the effect of griseofulvin.
  • Hydrocortisone The barbiturate, aprobarbital, may decrease the effect of the corticosteroid, hydrocortisone.
  • Levonorgestrel Phenobarbital decreases the effect of levonorgestrel
  • Medroxyprogesterone Acetate The enzyme inducer, aprobarbital, decreases the effect of the hormone agent, medroxyprogesterone.
  • Megestrol acetate The enzyme inducer, aprobarbital, decreases the effect of the hormone agent, megestrol.
  • Methadone The barbiturate, aprobarbital, decreases the effect of methadone.
  • Metronidazole The barbiturate, aprobarbital, decreases the effect of metronidazole.
  • Nifedipine The barbiturate, aprobarbital, decreases the effect of the calcium channel blocker, nifedipine.
  • Norethindrone This product may cause a slight decrease of contraceptive effect
  • Oxtriphylline The barbiturate, aprobarbital, decreases the effect of oxtriphylline.
  • Prednisolone The barbiturate, aprobarbital, may decrease the effect of the corticosteroid, prednisolone.
  • Prednisone The barbiturate, aprobarbital, may decrease the effect of the corticosteroid, prednisone.
  • Quinidine The anticonvulsant, aprobarbital, decreases the effect of quinidine.
  • Theophylline The barbiturate, aprobarbital, decreases the effect of theophylline.
  • Triamcinolone The barbiturate, aprobarbital, may decrease the effect of the corticosteroid, triamcinolone.
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