Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
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 hòa tan
1980 mg/L (at 25 °C)
pKa (strongest acidic)
8.75
Refractivity
49.15 m3·mol-1
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.