Tìm theo
Heptabarbital
Các tên gọi khác (10 ) :
  • Heptabarb
  • Heptabarbital
  • Heptabarbitone
  • Heptabarbum
  • Heptadorm
  • Heptamal
  • Heptamalum
  • Heptbarbital
  • Medapan
  • Medomine
barbiturates
Thuốc Gốc
Small Molecule
CAS: 509-86-4
ATC: N05CA11
CTHH: C13H18N2O3
PTK: 250.2936
Heptabarbital is an intermediate or short term barbiturate used mainly for sedation and hypnosis.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C13H18N2O3
Phân tử khối
250.2936
Monoisotopic mass
250.131742452
InChI
InChI=1S/C13H18N2O3/c1-2-13(9-7-5-3-4-6-8-9)10(16)14-12(18)15-11(13)17/h7H,2-6,8H2,1H3,(H2,14,15,16,17,18)
InChI Key
InChIKey=PAZQYDJGLKSCSI-UHFFFAOYSA-N
IUPAC Name
5-(cyclohept-1-en-1-yl)-5-ethyl-1,3-diazinane-2,4,6-trione
Traditional IUPAC Name
heptabarbital
SMILES
CCC1(C(=O)NC(=O)NC1=O)C1=CCCCCC1
Độ tan chảy
174
Độ hòa tan
250 mg/L (at 25 °C)
logP
2.03
logS
-2.9
pKa (strongest acidic)
8.14
PSA
75.27 Å2
Refractivity
66.25 m3·mol-1
Polarizability
25.86 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
3
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Cơ Chế Tác Dụng : Heptabarbital is an intermediate or short term barbiturate used mainly for sedation and hypnosis. Heptabarbital (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. Heptabarbital also appears to bind neuronal nicotinic acetylcholine receptors.
Dược Động Học :

▧ Metabolism :
Hepatic.
Độc Tính : Symptoms of an overdose typically include sluggishness, incoordination, difficulty in thinking, slowness of speech, faulty judgment, drowsiness or coma, shallow breathing, staggering, and in severe cases coma and death.
Chỉ Định : Used mainly for sedation and hypnosis.
Tương Tác Thuốc :
  • Aminophylline The barbiturate, heptabarbital, decreases the effect of aminophylline.
  • Betamethasone The barbiturate, heptabarbital, may decrease the effect of the corticosteroid, betamethasone.
  • Clomifene The enzyme inducer, heptabarbital, decreases the effect of the hormone agent, clomifene.
  • Conjugated Estrogens The enzyme inducer, heptabarbital, decreases the effect of the hormone agent, conjugated estrogens.
  • Cyclosporine The barbiturate, heptabarbital, increases the effect of cyclosporine.
  • Dexamethasone The barbiturate, heptabarbital, may decrease the effect of the corticosteroid, dexamethasone.
  • Diethylstilbestrol The enzyme inducer, heptabarbital, decreases the effect of the hormone agent, diethylstilbestrol.
  • Doxycycline The anticonvulsant, heptabarbital, decreases the effect of doxycycline.
  • Estradiol The enzyme inducer, heptabarbital, decreases the effect of the hormone agent, estradiol.
  • Ethinyl Estradiol This product may cause a slight decrease of contraceptive effect
  • Felodipine The barbiturate, heptabarbital, decreases the effect of felodipine.
  • Fludrocortisone The barbiturate, heptabarbital, may decrease the effect of the corticosteroid, fludrocortisone.
  • Folic Acid Folic acid decreases the effect of anticonvulsant, heptabarbital.
  • Gefitinib The CYP3A4 inducer, heptabarbital, may decrease the serum concentration and therapeutic effects of gefitinib.
  • Griseofulvin The barbiturate, heptabarbital, decreases the effect of griseofulvin.
  • Hydrocortisone The barbiturate, heptabarbital, may decrease the effect of the corticosteroid, hydrocortisone.
  • Levonorgestrel Phenobarbital decreases the effect of levonorgestrel
  • Medroxyprogesterone Acetate The enzyme inducer, heptabarbital, decreases the effect of the hormone agent, medroxyprogesterone.
  • Megestrol acetate The enzyme inducer, heptabarbital, decreases the effect of the hormone agent, megestrol.
  • Methadone The barbiturate, heptabarbital, decreases the effect of methadone.
  • Metronidazole The barbiturate, heptabarbital, decreases the effect of metronidazole.
  • Nifedipine The barbiturate, heptabarbital, decreases the effect of the calcium channel blocker, nifedipine.
  • Norethindrone This product may cause a slight decrease of contraceptive effect
  • Oxtriphylline The barbiturate, heptabarbital, decreases the effect of oxtriphylline.
  • Prednisolone The barbiturate, heptabarbital, may decrease the effect of the corticosteroid, prednisolone.
  • Prednisone The barbiturate, heptabarbital, may decrease the effect of the corticosteroid, prednisone.
  • Quinidine The anticonvulsant, heptabarbital, decreases the effect of quinidine.
  • Theophylline The barbiturate, heptabarbital, decreases the effect of theophylline.
  • Triamcinolone The barbiturate, heptabarbital, may decrease the effect of the corticosteroid, triamcinolone.
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : Geigy
    Sản phẩm biệt dược : Medomin
  • Công ty : Ciba
    Sản phẩm biệt dược : Medomine
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01354
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=10518
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508321
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C17725
ChemSpider
http://www.chemspider.com/Chemical-Structure.10081.html
PharmGKB
http://www.pharmgkb.org/drug/PA164783812
Wikipedia
http://en.wikipedia.org/wiki/Heptabarbital
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