Methaqualone: Difference between revisions

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==Pharmacology==

Despite prior speculation, a 2015 study demonstrates that methaqualone exhibits distinct functional properties at the [[GABA]] [[receptor]] sites compared with other allosteric modulators, and it mediates these through a different mechanism than the [[barbiturates]] and [[benzodiazepines]] that it historically has been lumped together with.<ref name="ncbi qualuude study">A Multifaceted GABAA Receptor Modulator: Functional Properties and Mechanism of Action of the Sedative-Hypnotic and Recreational Drug Methaqualone (Quaalude) (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/26056160</ref>

Despite prior speculation, a 2015 study demonstrates that methaqualone exhibits distinct functional properties at the [[GABA]] [[receptor]] sites compared with other allosteric modulators, and it mediates these through a different mechanism than the [[barbiturates]] and [[benzodiazepines]] that it historically has been lumped together with.<ref name="ncbi qualuude study">A Multifaceted GABAA Receptor Modulator: Functional Properties and Mechanism of Action of the Sedative-Hypnotic and Recreational Drug Methaqualone (Quaalude) (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/26056160</ref> These distinctions could contribute to the reported differences in the in vivo effects induced by methaqualone and classic CNS [[depressants]]. In any case, the multifaceted functionality of methaqualone at [[GABA#Drugs_targeting_GABA-A|GABA<sub>A</sub>]] receptors seems to be at the root of its clinical efficacy, as well as the addiction liability and recreational use associated with the drug.<ref name="ncbi qualuude study" />

~~These distinctions could contribute to~~ the ~~reported differences in the in vivo effects induced~~ by ~~methaqualone~~ and ~~classic CNS [[depressants]]~~. ~~In any case,~~ the ~~multifaceted functionality~~ of ~~methaqualone at [[~~GABA~~#Drugs_targeting_GABA-A|GABA<sub>A</sub>]]~~ receptors ~~seems to be at~~ the ~~root of its clinical efficacy~~, as ~~well~~ as ~~the addiction liability~~ and ~~recreational use associated with the drug~~.<ref ~~name~~=~~"ncbi qualuude study"~~ />

Methaqualone is a member of the class of quinazolines that is quinazolin-4-one substituted at positions 2 and 3 by methyl and o-tolyl groups respectively. A depressant that increases the activity of the GABA receptors in the brain and nervous system, it is used as a sedative and hypnotic medication. It has a role as a GABA agonist and a sedative.<ref>http://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:6821</ref>

It could be speculated that despite differences in targeted receptors, methaqualone essentially produces a variety of effects by binding to its receptor sites and magnifying the efficiency and effects of the [[neurotransmitter]] gamma aminobutyric acid (GABA) by acting on its receptors. As this site is the most prolific inhibitory receptor set within the brain, its modulation would explain the resulting [[sedating]] or [[anxiety suppression|calming]] effects which ensue.

@@ Line 9: / Line 9: @@
 ==Pharmacology==
-Despite prior speculation, a 2015 study demonstrates that methaqualone exhibits distinct functional properties at the [[GABA]] [[receptor]] sites compared with other allosteric modulators, and it mediates these through a different mechanism than the [[barbiturates]] and [[benzodiazepines]] that it historically has been lumped together with.<ref name="ncbi qualuude study">A Multifaceted GABAA Receptor Modulator: Functional Properties and Mechanism of Action of the Sedative-Hypnotic and Recreational Drug Methaqualone (Quaalude) (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/26056160</ref>
+Despite prior speculation, a 2015 study demonstrates that methaqualone exhibits distinct functional properties at the [[GABA]] [[receptor]] sites compared with other allosteric modulators, and it mediates these through a different mechanism than the [[barbiturates]] and [[benzodiazepines]] that it historically has been lumped together with.<ref name="ncbi qualuude study">A Multifaceted GABAA Receptor Modulator: Functional Properties and Mechanism of Action of the Sedative-Hypnotic and Recreational Drug Methaqualone (Quaalude) (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/26056160</ref> These distinctions could contribute to the reported differences in the in vivo effects induced by methaqualone and classic CNS [[depressants]]. In any case, the multifaceted functionality of methaqualone at [[GABA#Drugs_targeting_GABA-A|GABA<sub>A</sub>]] receptors seems to be at the root of its clinical efficacy, as well as the addiction liability and recreational use associated with the drug.<ref name="ncbi qualuude study" />
-These distinctions could contribute to the reported differences in the in vivo effects induced by methaqualone and classic CNS [[depressants]]. In any case, the multifaceted functionality of methaqualone at [[GABA#Drugs_targeting_GABA-A|GABA<sub>A</sub>]] receptors seems to be at the root of its clinical efficacy, as well as the addiction liability and recreational use associated with the drug.<ref name="ncbi qualuude study" />
+Methaqualone is a member of the class of quinazolines that is quinazolin-4-one substituted at positions 2 and 3 by methyl and o-tolyl groups respectively. A depressant that increases the activity of the GABA receptors in the brain and nervous system, it is used as a sedative and hypnotic medication. It has a role as a GABA agonist and a sedative.<ref>http://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:6821</ref>
 It could be speculated that despite differences in targeted receptors, methaqualone essentially produces a variety of effects by binding to its receptor sites and magnifying the efficiency and effects of the [[neurotransmitter]] gamma aminobutyric acid (GABA) by acting on its receptors. As this site is the most prolific inhibitory receptor set within the brain, its modulation would explain the resulting [[sedating]] or [[anxiety suppression|calming]] effects which ensue.