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What is Diclazepam?
Diclazepam is basically a synthetic depressant substance that belongs to a chemical class of benzodiazapines, and is related to diazepam in its properties.
The benzodiazepines contain a basic benzene ring that is linked with a seven membered diazepine ring, having two nitrogen constituents located at R1 and R4. Chemically, the Diclazepam has same structure, instead at R1 position, the Diclazepam is replaced with a methyl group.
The benzodiazepine ring is linked to a ring of 2-chlorinated phenyl at R5, and also a chlorine group is attached at R7 of benzyl ring. The Diclazepam also contains a ketone group that is formed by the double bonding of oxygen group to diazepine ring at R2 position.
This characteristic oxygen substitution at R2 position is similar in all benzodiazepine drugs, hence the suffix ?azepam is given to them.
In 1960 at Hoffman-La Roche, Leo Sternbach with his team work together to first conduct its synthesizes.
At present, it is only accessible through online as a research chemical. It is currently not available in market as a medicated compound because extensive investigations of potency after administration in humans aren?t been analyzed, though its two metabolites were found to be closely related to lometazepam, and potency value of ?10 greater than diazepam.
It has low toxicity relative to dose but it is an extremely potent drug, so it is dispensed as volumetric liquid dosing in a non-polar solvent to avoid inaccurate dosing and expected harm is reduced. It becomes poisonous when mixed with other depressants like opioids or alcohol.
As it belongs to benzodiazepine class, it shares the same physically and psychologically addictive and tolerance potential, so sudden discontinuation of Diclazepam produces life-threatening withdrawal symptoms. So, it is advisable that taper one dose gradually by lowering the quantity taken each day over a span of time.
Bioactivity of Diclazepam
The Diclazepam is related to diazepam and is considered its structural analogue. But, this compound has proven to be 10 times more potent than diazepam in animal models.
It has a wide range of activities on nervous system and acts to produce hypnosis, sedation, skeletal muscle relaxation, disinhibition, anxiety suppression and anticonvulsant effects and also possesses amnestic properties.
The mechanism of action of benzodiazepines is to induce effects by binding to a benzodiazepine receptor site, that is likely to enhance the activity of a neurotransmitter GABA (Gamma Aminobutyric acid) on its
receptor sites. As it is known that this receptor site is the most abundant inhibitory set present in brain nervous system, this results in immediate sedative effect of Diclazepam.
The anti-convulsant effect exhibited by Diclazepam is based on mechanism other than binding to benzodiazepines receptors site, as it tends to bind to voltage-dependant sodium (Na) channel either completely or partially.