![Pyrazolo[3,4-b]pyridine, the base chemical structure of this class. Pyrazolopyridine.png](http://upload.wikimedia.org/wikipedia/commons/thumb/3/31/Pyrazolopyridine.png/200px-Pyrazolopyridine.png)
The pyrazolopyridines are a group of drugs investigated as anxiolytics which act as positive allosteric modulators of the GABAA receptor via the barbiturate binding site. [1] [2] They include the following compounds:
Hypnotic, or soporific drugs, commonly known as sleeping pills, are a class of psychoactive drugs whose primary function is to induce sleep and to treat insomnia (sleeplessness).
Sodium thiopental, also known as Sodium Pentothal, thiopental, thiopentone, or Trapanal, is a rapid-onset short-acting barbiturate general anesthetic. It is the thiobarbiturate analog of pentobarbital, and an analog of thiobarbital. Sodium thiopental was a core medicine in the World Health Organization's List of Essential Medicines, but was supplanted by propofol. Despite this, thiopental is listed as an acceptable alternative to propofol, depending on local availability and cost of these agents. It was previously the first of three drugs administered during most lethal injections in the United States, but the US manufacturer Hospira stopped manufacturing the drug in 2011 and the European Union banned the export of the drug for this purpose. Although thiopental abuse carries a dependency risk, its recreational use is rare.
Picrotoxin, also known as cocculin, is a poisonous crystalline plant compound. It was first isolated by the French pharmacist and chemist Pierre François Guillaume Boullay (1777–1869) in 1812. The name "picrotoxin" is a combination of the Greek words "picros" (bitter) and "toxicon" (poison). A mixture of two different compounds, picrotoxin occurs naturally in the fruit of the Anamirta cocculus plant, although it can also be synthesized chemically.
Phenobarbital, also known as phenobarbitone or phenobarb, sold under the brand name Luminal among others, is a medication of the barbiturate type. It is recommended by the World Health Organization (WHO) for the treatment of certain types of epilepsy in developing countries. In the developed world, it is commonly used to treat seizures in young children, while other medications are generally used in older children and adults. In developed countries it is used for veterinary purposes. It may be used intravenously, injected into a muscle, or taken by mouth. The injectable form may be used to treat status epilepticus. Phenobarbital is occasionally used to treat trouble sleeping, anxiety, and drug withdrawal and to help with surgery. It usually begins working within five minutes when used intravenously and half an hour when administered by mouth. Its effects last for between four hours and two days.
Talbutal (Lotusate) is a barbiturate with a short to intermediate duration of action. It is a structural isomer of butalbital. Talbutal is a schedule III drug in the U.S.
Butabarbital is a prescription barbiturate sleep aid and anxiety medication. Butabarbital has a particularly fast onset of effects and short duration of action compared to other barbiturates, which makes it useful for certain applications such as treating severe insomnia, relieving general anxiety and relieving anxiety before surgical procedures; however it is also relatively dangerous particularly when combined with alcohol, and so is now rarely used, although it is still prescribed in some Eastern European and South American countries. Its intermediate duration of action gives butabarbital an abuse potential slightly lower than secobarbital. Butabarbital can be hydrolyzed to Valnoctamide.
Heptabarb, also known as heptabarbitone (BAN) or heptabarbital, is a sedative and hypnotic drug of the barbiturate family. It was used in Europe for the treatment of insomnia from the 1950s onwards, but has since been discontinued.
Phenacemide, also known as phenylacetylurea, is an anticonvulsant of the ureide (acetylurea) class. It is a congener and ring-opened analogue of phenytoin, and is structurally related to the barbiturates and to other hydantoins. Phenacemide was introduced in 1949 for the treatment of epilepsy, but was eventually withdrawn due to toxicity.
Mebutamate is an anxiolytic and sedative drug with antihypertensive effects of the carbamate class. It has effects comparable to those of barbiturates such as secobarbital, but is only around 1/3 the potency of secobarbital as a sedative. Side effects include dizziness and headaches.
Apronal, or apronalide, also known as allylisopropylacetylurea or allylisopropylacetylcarbamide, is a hypnotic/sedative drug of the ureide (acylurea) group synthesized in 1926 by Hoffmann-La Roche that is no longer used except in Japan. Though it is not a barbiturate, apronalide is similar in structure to the barbiturates. In accordance, it is similar in action to the barbiturates, although considerably milder in comparison. Upon the finding that it caused patients to develop thrombocytopenic purpura, apronalide was withdrawn from clinical use.
Etamivan is a respiratory stimulant drug related to nikethamide. It was mainly used in the treatment of barbiturate overdose and chronic obstructive pulmonary disease, but has now largely fallen into disuse.
Etazolate (SQ-20,009, EHT-0202) is an anxiolytic drug which is a pyrazolopyridine derivative and has unique pharmacological properties. It acts as a positive allosteric modulator of the GABAA receptor at the barbiturate binding site, as an adenosine antagonist of the A1 and A2 subtypes, and as a phosphodiesterase inhibitor selective for the PDE4 isoform. It is currently in clinical trials for the treatment of Alzheimer's disease.
Barbiturates are a class of depressant drugs that are chemically derived from barbituric acid. They are effective when used medically as anxiolytics, hypnotics, and anticonvulsants, but have physical and psychological addiction potential as well as overdose potential among other possible adverse effects. They have been been used recreationally for their anxiolytic and sedative effects, and are thus controlled in most countries due to the risks associated with such use.
Fenpentadiol (INN), also known as phenpentanediol, is a drug described as a tranquilizer and antidepressant that was formerly marketed in Europe. It also has stimulant, sedative, and anxiolytic effects, with the latter two occurring only at higher doses.
Barbiturate overdose is poisoning due to excessive doses of barbiturates. Symptoms typically include difficulty thinking, poor coordination, decreased level of consciousness, and a decreased effort to breathe. Complications of overdose can include noncardiogenic pulmonary edema. If death occurs this is typically due to a lack of breathing.
Barbiturate dependence develops with regular use of barbiturates. This in turn may lead to a need for increasing doses of the drug to get the original desired pharmacological or therapeutic effect. Barbiturate use can lead to both addiction and physical dependence, and as such they have a high potential for excess or non-medical use, however, it does not affect all users. Management of barbiturate dependence involves considering the affected person's age, comorbidity and the pharmacological pathways of barbiturates.
Cartazolate (SQ-65,396) is a drug of the pyrazolopyridine class. It acts as a GABAA receptor positive allosteric modulator at the barbiturate binding site of the complex and has anxiolytic effects in animals. It is also known to act as an adenosine antagonist at the A1 and A2 subtypes and as a phosphodiesterase inhibitor. Cartazolate was tested in human clinical trials and was found to be efficacious for anxiety but was never marketed. It was developed by a team at E.R. Squibb and Sons in the 1970s.
Thiotetrabarbital is a drug which is a short-acting barbiturate derivative that is used as an anesthetic. It has been used in veterinary medicine.
In pharmacology, GABAA receptor positive allosteric modulators are positive allosteric modulator (PAM) molecules that increase the activity of the GABAA receptor protein in the vertebrate central nervous system.
Metallibure (INN), also known as methallibure or methallibur (German), is a medication which was introduced in 1973 and has been used in veterinary medicine to synchronize estrus. It was withdrawn in the United States and Europe due to teratogenicity and has been replaced with altrenogest, a progestin.
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