Diproqualone is a
quinazolinone class
GABAergic
In molecular biology and physiology, something is GABAergic or GABAnergic if it pertains to or affects the neurotransmitter gamma-aminobutyric acid (GABA). For example, a synapse is GABAergic if it uses GABA as its neurotransmitter, and a GABAergic ...
and is an analogue of
methaqualone
Methaqualone is a hypnotic sedative. It was sold under the brand names Quaalude ( ) and Sopor among others, which contained 300 mg of methaqualone, and sold as a combination drug under the brand name Mandrax, which contained 250 mg me ...
developed in the late 1950s by a team at Nogentaise de Produits Chimique. It was marketed primarily in France and some other European countries.
It has
sedative
A sedative or tranquilliser is a substance that induces sedation by reducing irritability or Psychomotor agitation, excitement. They are central nervous system (CNS) Depressant, depressants and interact with brain activity, causing its decelera ...
,
anxiolytic
An anxiolytic (; also antipanic or anti-anxiety agent) is a medication or other intervention that reduces anxiety. This effect is in contrast to anxiogenic agents which increase anxiety. Anxiolytic medications are used for the treatment of anxie ...
,
antihistamine
Antihistamines are drugs which treat allergic rhinitis, common cold, influenza, and other allergies. Typically, people take antihistamines as an inexpensive, generic (not patented) drug that can be bought without a prescription and provides ...
and
analgesic
An analgesic drug, also called simply an analgesic, antalgic, pain reliever, or painkiller, is any member of the group of drugs used for pain management. Analgesics are conceptually distinct from anesthetics, which temporarily reduce, and in s ...
properties, resulting from its agonist activity at the β subtype of the
GABAa receptor, antagonist activity at all
histamine receptor
The histamine receptors are a class of G protein–coupled receptors which bind histamine as their primary endogenous ligand. Histamine is a neurotransmitter involved in various physiological processes. There are four main types of histamine recep ...
s, inhibition of the
cyclooxygenase-1
Cyclooxygenase 1 (COX-1), also known as prostaglandin-endoperoxide synthase 1 (Human Genome Organisation, HUGO PTGS1), is an enzyme that in humans is encoded by the ''PTGS1'' gene. In humans it is one of Cyclooxygenase-3, three cyclooxygenases.
...
enzyme, and possibly its agonist activity at both the
sigma-1 receptor
The sigma-1 receptor (σ1R), one of two sigma receptor subtypes, is a Chaperone (protein), chaperone protein at the endoplasmic reticulum (ER) that modulates calcium signaling through the IP3 receptor. In humans, the σ1 receptor is encoded by ...
and
sigma-2 receptor (the function of these receptors and their clinical relevance has not yet been determined). Diproqualone is used primarily for treating inflammatory pain associated with osteoarthritis and rheumatoid arthritis and more rarely, for treating insomnia, anxiety and neuralgia.
Diproqualone is the only analogue of methaqualone that is still in widespread clinical use, due to its useful anti-inflammatory and analgesic effects in addition to the sedative and anxiolytic actions common to other drugs of this class. There are still some concerns about the potential of diproqualone for abuse and overdose. So, it is not sold as a pure drug but only as the camphosulfonate salt in combination mixtures with other medicines such as
ethenzamide.
See also
*
Afloqualone
Afloqualone (Arofuto) is a quinazolinone family GABAergic drug and is an analogue of methaqualone developed in the 1970s by a team at Tanabe Seiyaku. It has sedative and muscle-relaxant effects resulting from its agonist activity at the β subt ...
*
Etaqualone
Etaqualone (Aolan, Athinazone, Ethinazone) is a quinazolinone-class GABAergic and is an analogue of methaqualone that was developed in the 1960s. It was primarily marketed in France and other European countries, as well as later in China, where ...
*
Methylmethaqualone
*
Mecloqualone
Mecloqualone (Nubarene, Casfen) is a quinazolinone-class GABAergic and is an analogue of methaqualone that was first made in 1960 and marketed mainly in France and some other European countries. It has sedative, hypnotic, and anxiolytic properti ...
*
Mebroqualone
Mebroqualone (MBQ) is a quinazolinone-class GABAergic and is an analogue of mecloqualone that has similar sedative and hypnotic properties to its parent compound, resulting from its agonist activity at the β subtype of the GABAa receptor. It w ...
*
Cloroqualone
Cloroqualone is a quinazolinone-class GABAergic and is an analogue of methaqualone developed in the 1980s and marketed mainly in France and some other European countries. It has sedative and antitussive properties resulting from its agonist act ...
*
Gamma-Aminobutyric acid
GABA (gamma-aminobutyric acid, γ-aminobutyric acid) is the chief inhibitory neurotransmitter in the developmentally mature mammalian central nervous system. Its principal role is reducing neuronal excitability throughout the nervous system.
GA ...
References
Sedatives
Analgesics
Diols
Quinazolinones
GABAA receptor positive allosteric modulators
Lactams
{{sedative-stub