Tìm theo
Metharbital
Các tên gọi khác (3) :
  • Metarbital
  • Metharbital
  • Metharbitalum
Thuốc Gốc
Small Molecule
CAS: 50-11-3
ATC: N03AA30
CTHH: C9H14N2O3
PTK: 198.2191
Metharbital was patented in 1905 by Emil Fischer working for Merck. It was marketed as Gemonil by Abbott Laboratories. It is a barbiturate anticonvulsant, used in the treatment of epilepsy. It has similar properties to phenobarbital [Wikipedia].
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
Phân tử khối
198.2191
Monoisotopic mass
198.100442324
InChI
InChI=1S/C9H14N2O3/c1-4-9(5-2)6(12)10-8(14)11(3)7(9)13/h4-5H2,1-3H3,(H,10,12,14)
InChI Key
InChIKey=FWJKNZONDWOGMI-UHFFFAOYSA-N
IUPAC Name
5,5-diethyl-1-methyl-1,3-diazinane-2,4,6-trione
Traditional IUPAC Name
metharbital
SMILES
CCC1(CC)C(=O)NC(=O)N(C)C1=O
Độ tan chảy
150.5 °C
Độ hòa tan
1980 mg/L (at 25 °C)
logP
1.15
logS
-2.23
pKa (strongest acidic)
8.75
PSA
66.48 Å2
Refractivity
49.15 m3·mol-1
Polarizability
19.6 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
3
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
1
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
8.01 (at 25 °C)
Dược Lực Học : Metharbital, a barbiturate, is used for the treatment of short term insomnia. It belongs to a group of medicines called central nervous system (CNS) depressants that induce drowsiness and relieve tension or nervousness. Little analgesia is conferred by barbiturates; their use in the presence of pain may result in excitation.
Cơ Chế Tác Dụng : Metharbital was patented in 1905 by Emil Fischer working for Merck. It was marketed as Gemonil by Abbott Laboratories. It is a barbiturate anticonvulsant, used in the treatment of epilepsy. It has similar properties to phenobarbital [Wikipedia]. Metharbital binds at a distinct binding site associated with a Cl- ionopore at the GABAA receptor, increasing the duration of time for which the Cl- ionopore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged. All of these effects are associated with marked decreases in GABA-sensitive neuronal calcium conductance (gCa). The net result of barbiturate action is acute potentiation of inhibitory GABAergic tone. Barbiturates also act through potent (if less well characterized) and direct inhibition of excitatory AMPA-type glutamate receptors, resulting in a profound suppression of glutamatergic neurotransmission.
Độc Tính : Signs of overdose include confusion (severe), decrease in or loss of reflexes, drowsiness (severe), fever, irritability (continuing), low body temperature, poor judgment, shortness of breath or slow or troubled breathing, slow heartbeat, slurred speech, staggering, trouble in sleeping, unusual movements of the eyes, weakness (severe).
Chỉ Định : Metharbital is used for the treatment of epilepsy.
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