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KI0775DiazepamQuoteQuote

Chemical Characteristic

Product NameDiazepam
SynonymsValium, Dizac
CAS No.439-14-5
Molecular Weight 284.74
FormulaC16H13ClN2O
Chemical Name7-Chloro-1,3-dihydro-1-methyl-5-phenyl-2H-1,4-benzodiazepin-2-one
SmilesN1(C(=O)CN=C(c2c1ccc(c2)Cl)c1ccccc1)C
Chemical Structure

Biological activities

Diazepam binds to a specific subunit on the GABAA receptor at the allosteric site. Diazepam has a wide therapeutic application as anxiolytics, anticonvulsants and muscle relaxants. Diazepam inhibits contractions of ileal longitudinal muscle strips with an ED50 of 13µM and an IC50 of 113 nM. [1] Diazepam (10 µM) significantly potentiates the presynaptic inhibitory action of adenosine on both the twitch and sustained response, with IC50 of 2 and 45 µM, respectively. The potentiation of adenosine by diazepam is due to an inhibition of adenosine uptake. [2] Diazepam appears to bind specifically to a single, saturable, binding site located on rat brain membranes, with an affinity constant near 3 nM at pH 7.4.[3] In vivo, 5 mg/kg diazepam decreases dopamine to about 75% and attenuates the novelty- and handling-induced increases in Wistar rats.[4]

Protocols

Diazepam is diluted in methanol.[1]

References

[1] Hullihan JP, et al. The binding of [3H]-diazepam to guinea-pigileal longitudinal muscle and the in vitro inhibition of contraction by benzodiazepines. Br J Pharmacol. 1983, 78 (2): 321-327.
[2] Clanachan AS, et al. Potentiation of the effects of adenosine on isolated cardiac and smooth muscle by diazepam. Br J Pharmacol. 1980, 71(2): 459-466.
[3] Braestrup C, et al. Specific benzodiazepine receptors in rat brain characterized by high-affinity (3H) diazepam binding. Proc Natl Sci USA. 1977, 74(9): 3805-3809.
[4] Feenstra MG, et al. Novelty-induced increase in dopamine release in the rat prefrontal cortex in vivo: inhibition by diazepam. Neurosci Lett. 1995, 182(2): 81-84.

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