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Pregabalin

Pregabalin
Drug information
Systematic (IUPAC) name
IUPAC name(S)-3-(aminomethyl)-5-methylhexanoic acid
Chemical data
Mol. mass159.23 g.mol-1
Bioavailability≥90%
Protein bindingNil
MetabolismNegligible
Half-life5 � 6.5 hours
ExcretionRenal
Therapeutic considerations
Pregnancy cat B3 (Au), C (U.S.)
Legal status S4 (Au), POM (UK), Schedule V (U.S.)
RoutesOral(main), IV, Insufflation

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Pregabalin (INN) ( ) is an anticonvulsant drug used for neuropathic pain and as an adjunct therapy for partial seizures with or without secondary generalization in adults. It has also been found effective for generalized anxiety disorder and is (as of 2007) approved for this use in the European Union. It was designed as a more potent successor to gabapentin. Pregabalin is marketed by Pfizer under the trade name Lyrica. Pfizer described in a SEC filing that the drug could be used to treat epilepsy, post-herpetic neuralgia and diabetic peripheral neuropathy, fibromyalgia, et al. Sales reached record $3,063 million in 2010.

Recent studies have shown that pregabalin is effective at treating chronic pain in disorders such as fibromyalgia and spinal cord injury. In June 2007, pregabalin became the first medication approved by the U.S. Food and Drug Administration specifically for the treatment of fibromyalgia.

It is considered to have a low potential for abuse, and a limited dependence liability if misused, and is thus classified as a Schedule V drug in the U.S.

Lyrica is one of four drugs which a subsidiary of Pfizer in 2009 pleaded guilty to misbranding "with the intent to defraud or mislead". Pfizer agreed to pay $2.3 billion (£1.4 billion) in settlement, and entered a corporate integrity agreement. Pfizer illegally promoted the drugs and caused false claims to be submitted to government healthcare programs for uses that were not medically accepted.

Pregabalin is available in 25, 50, 75, 100, 150, 200, 225, and 300 mg capsules, and recently a strawberry flavoured oral solution has been developed, containing 20 mg/mL with an added sweetening agent (sucrose) to mask the chemical's bitter taste. The maximum daily recommended dose for pregabalin is 600 mg. Dosages must be monitored and increases should be based on patient's tolerance.

Pregabalin Video

Scientist VTB compaires the anxiety medication nuerontin to its supposed upgrade lyrica.Weighing the pros and cons of each
6.87 min. | 4.54 user rating
A pill used for nerve pain offers women relief from hot flashes, Mayo Clinic researchers report at the 45th Annual Meeting of the American Society of Clinical Oncology (ASCO). They say the agent, pregabalin, decreased hot flash severity and frequency about 20 percent more than did a placebo agent. Thus, pregabalin appears to offer about the same benefit as gabapentin, an older, related drug, as well as newer classes of antidepressants. Hot flashes are a major problem in many women, and for those who opt not to take hormonal therapies or antidepressants, pregabalin appears to be another treatment option, says the studys lead author, Charles Loprinzi, MD, a medical oncologist at the Mayo Clinic in Minnesota. While pregabalin offers about the same benefit as gabapentin, women who use it only need to take two pills a day, versus three for gabapentin, he says. Side effects can occur with the use of either drug. However, in this study, they were not severe enough that participants stopped using the active study drug any more often than did patients who were taking placebos, researchers say. Dr. Loprinzi has pioneered the field of nonhormonal hot flash therapy, which he began researching decades ago to help breast cancer patients using tamoxifen, an anti-estrogen treatment that creates symptoms of menopause. He is the first researcher to test the use of antidepressants, compared to placebo treatment, for hot flashes.
3.98 min. | 5.0 user rating
Buy pregabalin online on www.popularpillsonline.net - Buy generic lyrica online for BEST PRICE!!! Pregabalin is used to treat nerve pain from diabetes, shingles, and fibromyalgia. It is also used to control seizures in epilepsy. This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.
10.02 min. | 3.4 user rating
I periodi bui vanno esorcizzati, così come le malattie... dopo La Compagnia del Frollino ecco un video realizzato da Raffaele Giuria e Sebastiano Roncaglia. Based on a true story.
6.02 min. | 4.42 user rating
FDA is alerting healthcare professionals that the labeling for antiepileptic drugs will now warn that patients taking these drugs have an increased risk of suicidal thoughts and actions. The warnings are based on FDA's analysis of placebo-controlled clinical studies of eleven drugs used to treat epilepsy, psychiatric disorders and other conditions. In this analysis, the risk was approximately doubled in patients receiving the anti-epileptic drugs compared with those getting placebo -- 0.43% vs. 0.22%. The following drugs were included in the analyses: Carbamazepine (marketed as Carbatrol, Equetro, Tegretol, Tegretol XR) Felbamate (marketed as Felbatol) Gabapentin (marketed as Neurontin) Lamotrigine (marketed as Lamictal) Levetiracetam (marketed as Keppra) Oxcarbazepine (marketed as Trileptal) Pregabalin (marketed as Lyrica) Tiagabine (marketed as Gabitril) Topiramate (marketed as Topamax) Valproate (marketed as Depakote, Depakote ER, Depakene, Depacon) Zonisamide (marketed as Zonegran) The increased risk was seen as early as one week after starting therapy and continued through 24 weeks. And it was generally consistent for all eleven drugs in the analysis, and across a range of indications. This suggests that this risk applies to all antiepileptic drugs when they're used for any indication - even those that weren't part of the analysis. Healthcare professionals should closely monitor all patients starting or taking antiepileptic drugs. They should be alert to changes in <b>...</b>
1.43 min. | 4.0 user rating
normast.wordpress.com Palmitoylethanolamide (Normast), is a body own fatty compound, related to anandamide and proven to have analgesic activity in severe pain in many patients. Normast is in the Netherlands free available as a foodsupplement and the internet organization Ergomax exports Normast to some of our patients abroad without problems. This case was especially interesting, as recently it appeared that pregabalin was ineffective in the treatment of sciatic pain. Normast is registered in European contries as medical food and so far in our clinic we did not see any side effects. This patient too responded well to the addition of Normast to his treatment scedule. He could directly stop taking Lyrica. Normal dose of Normast is twice daily 600 mg, starting with granules sublingual for 10 days, then 10 days twice daily 600 mg tablets and in case of early response, decrease dose to twice daily 300 mg, otherwise keep going with twice daily 600 mg Normast up to 6 weeks. In our institute for neuropathic pain we treat many neuropathic pain patients with the natural compound Normast, available as a foodsupplement in the Netherlands and distributed by the organization Ergomax. Sciatic pain or sciatica Lumbosacral radicular pain is characterized by a radiating pain in one or more lumbar or sacral dermatomes; it may or may not be accompanied by other radicular irritation symptoms and/or symptoms of decreased function. The annual prevalence in the general population, described as <b>...</b>
4.20 min. | 5.0 user rating
A brief video describing the use of pregabalin also known as Lyrica for the treatment of fibromyalgia, chronic pain, and neuropathic pain.
1.82 min. | 5.0 user rating
www.superdrugsaver.org Lyrica (pregabalin) is an anti-epileptic drug, also called an anticonvulsant. It works by slowing down impulses in the brain that cause seizures. Lyrica also affects chemicals in the brain that send pain signals across the nervous system.Lyrica is used to control seizures...
1.08 min. | 5.0 user rating
Primary fibromyalgia is a common yet poorly understood syndrome characterized by diffuse chronic pain accompanied by other somatic symptoms, including poor sleep, fatigue, and stiffness, in the absence of disease. Fibromyalgia does not have a distinct cause or pathology. www.comlexflashcards.com
2.88 min. | 5.0 user rating

4.80 min. | 5.0 user rating

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New Guideline Suggest Treatments for Diabetes - TopNews New Zealand Tweet this news
TopNews New Zealand--As per this fresh guideline, a drug, -pregabalin-, is capable of relieving intense nerve pain, the burning or tingling sensation in the hands and feet in majority of diabetic patients. It is, however, maintained that the drug cannot b - Date : Sat, 16 Apr 2011 10:34:39 GMT+00:00
Neurologists Issue New Guideline for Treating Neuropathy - Diabetes Health (press release) Tweet this news
Diabetes Health (press release)--The guideline says that the seizure drug -pregabalin- is effective in treating diabetic nerve pain and can improve quality of life. However, it notes that -pregabalin- may not be appropriate for all patients. The guideline - Date : Sat, 23 Apr 2011 13:01:17 GMT+00:00
Pregabalin May Benefit Diabetic Nerve Pain - eMaxHealth Tweet this news
eMaxHealth---Pregabalin-, brand name Lyrica, is an oral medication used for treating pain caused by neurologic diseases as well as seizures. It is also used for treating fibromyalgia. It is believed to work by binding to calcium channels on nerves and pos - Date : Thu, 14 Apr 2011 15:02:25 GMT+00:00
Relationships between changes in pain severity and other patient-reported ... - 7thSpace Interactive (press release) Tweet this news
7thSpace Interactive (press release)--Methods: This is a secondary analysis of a clinical trial evaluating -pregabalin- in patients with posttraumatic peripheral neuropathic pain (N=254). Regression models were used to determine associations between chang - Date : Fri, 25 Mar 2011 13:15:31 GMT+00:00
What is Lyrica and why is it buying me a new building? - North by Northwestern Tweet this news
North by Northwestern--In testing the molecule on mice, they found that this “-pregabalin-” (the scientific name for Lyrica) molecule had an ability to suppress seizures. After testing it and refining it, it was finally approved by the FDA in 2004 and - Date : Thu, 31 Mar 2011 18:19:33 GMT+00:00
Decision ResourcesPosted on:15 Mar 11 - PharmiWeb.com (press release) Tweet this news
PharmiWeb.com (press release)---...- percentages of surveyed neurologists (53 percent) and surveyed managed care organizations' (MCO) pharmacy directors (40 percent) chose Pfizer's Lyrica (-pregabalin-) as the most efficacious therapy, when comp - Date : Tue, 15 Mar 2011 14:05:36 GMT+00:00
New drug may help control seizures - Foster's Daily Democrat Tweet this news
Foster's Daily Democrat--A new drug, -Pregabalin-, has been shown in some small trials to add to the efficacy of the two standby drugs, and, in combination with one or both of them, ... - Date : Sun, 16 Jan 2011 08:24:28 GMT+00:00
Beacon NewsFlashes - January 25, 2011 - The AIDS Beacon Tweet this news
The AIDS Beacon---...- 3 clinical trial is currently recruiting participants to test the effectiveness of Lyrica (-pregabalin-) in treating pain from HIV-related neuropathy. ... - Date : Tue, 25 Jan 2011 22:24:45 GMT+00:00
DR ROSEMARY LEONARD: WHY CAN'T I BUY REGAINE - Express.co.uk Tweet this news
Express.co.uk--If you have pain, Amitriptyline, -pregabalin- or gabapentin, which regulate pain messages travelling to the brain, are much more effective than normal ... - Date : Tue, 25 Jan 2011 00:58:27 GMT+00:00
Pregabalin: Ärzte warnen vor Missbrauch - Pharmazeutische Zeitung online Tweet this news
Pharmazeutische Zeitung online--Die Arzneimittelkommission der Ärzteschaft macht auf das Missbrauchpotenzial von -Pregabalin- (Lyrica ® ) aufmerksam. Anlass ist der Fallbericht eines ... - Date : Mon, 31 Jan 2011 13:13:21 GMT+00:00

Anticonvulsants (N03)

GABAA receptor agonist
BarbituratesBarbexaclone * Metharbital * Methylphenobarbital * Pentobarbital * Phenobarbital# * Primidone
BenzodiazepinesClobazam * Clonazepam * Clorazepate * Diazepam# * Flutoprazepam * Lorazepam * Midazolam * Nimetazepam * Nitrazepam * Temazepam
Other GABA agents
Aromatic allylic alcoholsStiripentol
Carbonic anhydrase inhibitor
Sulfa drugsAcetazolamide * Ethoxzolamide * Sultiame * Zonisamide
Channel blockers

Anticonvulsants (N03)

GABAA receptor agonist
BarbituratesBarbexaclone * Metharbital * Methylphenobarbital * Pentobarbital * Phenobarbital# * Primidone
BenzodiazepinesClobazam * Clonazepam * Clorazepate * Diazepam# * Flutoprazepam * Lorazepam * Midazolam * Nimetazepam * Nitrazepam * Temazepam
Other GABA agents
Aromatic allylic alcoholsStiripentol
Carbonic anhydrase inhibitor
Sulfa drugsAcetazolamide * Ethoxzolamide * Sultiame * Zonisamide
Channel blockers
GABAA receptor agonist
BarbituratesBarbexaclone * Metharbital * Methylphenobarbital * Pentobarbital * Phenobarbital# * Primidone
BenzodiazepinesClobazam * Clonazepam * Clorazepate * Diazepam# * Flutoprazepam * Lorazepam * Midazolam * Nimetazepam * Nitrazepam * Temazepam
Other GABA agents
Aromatic allylic alcoholsStiripentol
Carbonic anhydrase inhibitor
Sulfa drugsAcetazolamide * Ethoxzolamide * Sultiame * Zonisamide
Channel blockers
subgroup |groupstyle=background-color: LemonChiffon |Primarily sodium |
HydantoinsEthotoin * Fosphenytoin * Mephenytoin * Phenytoin#
CarboxamidesCarbamazepine# * Eslicarbazepine acetate * Oxcarbazepine * Rufinamide

Analgesics (N02A, N02B)

Opioids
See also: Opioids template
Opium & alkaloids thereof Codeine * Morphine * Opium * Laudanum * Paregoric
Pyrazolones
Ampyrone/Aminophenazone * Metamizole * Phenazone * Propyphenazone
Cannabinoids
Ajulemic acid * AM404 * Cannabidiol * Cannabis * Nabilone * Nabiximols * Tetrahydrocannabinol
Anilides
Paracetamol (acetaminophen) * Phenacetin * Propacetamol
Non-steroidal
anti-inflammatories
See also: NSAIDs template
Propionic acid class Fenoprofen * Flurbiprofen * Ibuprofen * Ketoprofen * Naproxen * Oxaprozin
Atypical, adjunct and potentiators,
miscellaneous
Befiradol * Bicifadine * Camphor * Clonidine * Cyclobenzaprine * Duloxetine * Esreboxetine * Flupirtine * Gabapentin * Glafenine * Hydroxyzine * Menthol * Nefopam * Orphenadrine * Pregabalin * Scopolamine * Tebanicline * Trazodone * Ziconotide |belowstyle=background: LemonChiffon

Anxiolytics (N05B)

GABAA PAMs
BenzodiazepineAdinazolam * Alprazolam * Bretazenil * Bromazepam * Camazepam * Chlordiazepoxide * Clobazam * Clonazepam * Clorazepate * Clotiazepam * Cloxazolam * Diazepam * Ethyl Loflazepate * Etizolam * Fludiazepam * Halazepam * Imidazenil * Ketazolam * Lorazepam * Medazepam * Nordazepam * Oxazepam * Pinazepam * Prazepam
CarbamatesEmylcamate * Mebutamate * Meprobamate (Carisoprodol, Tybamate) * Phenprobamate * Procymate
NonbenzodiazepinesAbecarnil * Adipiplon * Alpidem * CGS-9896 * CGS-20625 * Divaplon * ELB-139 * Etifoxine * GBLD-345 * Gedocarnil * ICI-190,622 * L-838,417 * NS-2664 * NS-2710 * Ocinaplon * Pagoclone * Panadiplon * Pipequaline * RWJ-51204 * SB-205,384 * SL-651,498 * TP-003 * TP-13 * TPA-023 * Tracazolate * Y-23684 * ZK-93423
OthersChlormezanone * Etazolate * Ethanol (Alcohol) * Kavalactones (Kava Kava) * Skullcap * Valerenic Acid (Valerian)
α2δ VDCC Blockers
Gabapentin * Pregabalin
5-HT1A Agonists
Azapirones: Buspirone * Gepirone * Tandospirone; Others: Flesinoxan * Oxaflozane
H1 Antagonists
Diphenylmethanes: Captodiame * Hydroxyzine; Others: Brompheniramine * Chlorpheniramine * Pheniramine
CRF1 Antagonists
Antalarmin * CP-154,526 * Pexacerfont * Pivagabine
NK2 Antagonists
GR-159,897 * Saredutant
MCH1 antagonists
ATC-0175 * SNAP-94847
mGluR2/3 Agonists
Eglumegad
mGluR5 NAMs
Fenobam
TSPO agonists
DAA-1097 * DAA-1106 * Emapunil * FGIN-127 * FGIN-143
σ1 agonists
Afobazole * Opipramol
Others
Benzoctamine * Carbetocin * Demoxytocin * Mephenoxalone * Mepiprazole * Oxanamide * Oxytocin * Promoxolane * Tofisopam * Trimetozine * WAY-267,464 |belowstyle=background: LemonChiffon

Mood Stabilizers

Carbamazepine * Divalproex Sodium * Gabapentin * Lamotrigine * Licarbazepine * Lithium * Omega-3 Fatty Acids * Oxcarbazepine * Pregabalin * Sodium Valproate * Tiagabine * Topiramate * Valproic Acid

GABAergics

Receptor
Ligands
GABAAAgonists: Main Site: Bamaluzole * Gaboxadol * Ibotenic Acid * Isoguvacine * Isonipecotic Acid * Muscimol (Amanita Muscaria) * Progabide * SL 75102 * Thiomuscimol * Tolgabide; Positive Allosteric Modulators: Barbiturates * Benzodiazepines * Carbamates * Chlormezanone * Clomethiazole * Etazolate * Ethanol (Alcohol) * Etomidate * Kavalactones (Kava Kava) * Loreclezole * Neuroactive Steroids * Nonbenzodiazepines * Phenols * Piperidinediones * Propanidid * Quinazolinones * ROD-188 * Skullcap * Stiripentol * Thymol * Valerenic Acid (Valerian)
* See here for a full list of GABAA positive allosteric modulators.
Antagonists: Main Site: Bicuculline * Gabazine; Negative Allosteric Modulators: α5IA * Bilobalide * Cicutoxin * DMCM * Flumazenil * Flurothyl * Furosemide * L-655,708 * Oenanthotoxin * Penicillin * Pentylenetetrazol * Picrotoxin * Pitrazepin * PWZ-029 * Ro15-4513 * Sarmazenil * Suritozole * Thujone (Absinthe) * Thiocolchicoside
GABABAgonists: Main Site: 1,4-Butanediol * Baclofen * GBL * GHB * GHV * GVL * Phenibut * Progabide * SKF-97541 * Tolgabide; Positive Allosteric Modulators: BHF-177 * BHFF * BSPP * CGP-7930 * GS-39783
Antagonists: Main Site: CGP-35348 * Phaclofen * Saclofen * SCH-50911
GABACAgonists: Main Site: CACA * CAMP * GABOB * N(4)-chloroacetylcytosine arabinoside * Progabide * Tolgabide
Antagonists: Main Site: Bilobalide * TPMPA
Reuptake
Inhibitors

GABAergics

Receptor
Ligands
GABAAAgonists: Main Site: Bamaluzole * Gaboxadol * Ibotenic Acid * Isoguvacine * Isonipecotic Acid * Muscimol (Amanita Muscaria) * Progabide * SL 75102 * Thiomuscimol * Tolgabide; Positive Allosteric Modulators: Barbiturates * Benzodiazepines * Carbamates * Chlormezanone * Clomethiazole * Etazolate * Ethanol (Alcohol) * Etomidate * Kavalactones (Kava Kava) * Loreclezole * Neuroactive Steroids * Nonbenzodiazepines * Phenols * Piperidinediones * Propanidid * Quinazolinones * ROD-188 * Skullcap * Stiripentol * Thymol * Valerenic Acid (Valerian)
* See here for a full list of GABAA positive allosteric modulators.
Antagonists: Main Site: Bicuculline * Gabazine; Negative Allosteric Modulators: α5IA * Bilobalide * Cicutoxin * DMCM * Flumazenil * Flurothyl * Furosemide * L-655,708 * Oenanthotoxin * Penicillin * Pentylenetetrazol * Picrotoxin * Pitrazepin * PWZ-029 * Ro15-4513 * Sarmazenil * Suritozole * Thujone (Absinthe) * Thiocolchicoside
GABABAgonists: Main Site: 1,4-Butanediol * Baclofen * GBL * GHB * GHV * GVL * Phenibut * Progabide * SKF-97541 * Tolgabide; Positive Allosteric Modulators: BHF-177 * BHFF * BSPP * CGP-7930 * GS-39783
Antagonists: Main Site: CGP-35348 * Phaclofen * Saclofen * SCH-50911
GABACAgonists: Main Site: CACA * CAMP * GABOB * N(4)-chloroacetylcytosine arabinoside * Progabide * Tolgabide
Antagonists: Main Site: Bilobalide * TPMPA
Reuptake
Inhibitors
Receptor
Ligands
GABAAAgonists: Main Site: Bamaluzole * Gaboxadol * Ibotenic Acid * Isoguvacine * Isonipecotic Acid * Muscimol (Amanita Muscaria) * Progabide * SL 75102 * Thiomuscimol * Tolgabide; Positive Allosteric Modulators: Barbiturates * Benzodiazepines * Carbamates * Chlormezanone * Clomethiazole * Etazolate * Ethanol (Alcohol) * Etomidate * Kavalactones (Kava Kava) * Loreclezole * Neuroactive Steroids * Nonbenzodiazepines * Phenols * Piperidinediones * Propanidid * Quinazolinones * ROD-188 * Skullcap * Stiripentol * Thymol * Valerenic Acid (Valerian)
* See here for a full list of GABAA positive allosteric modulators.
Antagonists: Main Site: Bicuculline * Gabazine; Negative Allosteric Modulators: α5IA * Bilobalide * Cicutoxin * DMCM * Flumazenil * Flurothyl * Furosemide * L-655,708 * Oenanthotoxin * Penicillin * Pentylenetetrazol * Picrotoxin * Pitrazepin * PWZ-029 * Ro15-4513 * Sarmazenil * Suritozole * Thujone (Absinthe) * Thiocolchicoside
GABABAgonists: Main Site: 1,4-Butanediol * Baclofen * GBL * GHB * GHV * GVL * Phenibut * Progabide * SKF-97541 * Tolgabide; Positive Allosteric Modulators: BHF-177 * BHFF * BSPP * CGP-7930 * GS-39783
Antagonists: Main Site: CGP-35348 * Phaclofen * Saclofen * SCH-50911
GABACAgonists: Main Site: CACA * CAMP * GABOB * N(4)-chloroacetylcytosine arabinoside * Progabide * Tolgabide
Antagonists: Main Site: Bilobalide * TPMPA
Reuptake
Inhibitors
subgroup |groupstyle=background-color: LightYellow |Plasmalemmal |
GAT InhibitorsCI-966 * Deramciclane * EF-1502 * Gabaculine * Guvacine * Nipecotic acid * NNC 05-2090 * SKF-89976A * SNAP-5114 * Tiagabine

GABAergics

Receptor
Ligands
GABAAAgonists: Main Site: Bamaluzole * Gaboxadol * Ibotenic Acid * Isoguvacine * Isonipecotic Acid * Muscimol (Amanita Muscaria) * Progabide * SL 75102 * Thiomuscimol * Tolgabide; Positive Allosteric Modulators: Barbiturates * Benzodiazepines * Carbamates * Chlormezanone * Clomethiazole * Etazolate * Ethanol (Alcohol) * Etomidate * Kavalactones (Kava Kava) * Loreclezole * Neuroactive Steroids * Nonbenzodiazepines * Phenols * Piperidinediones * Propanidid * Quinazolinones * ROD-188 * Skullcap * Stiripentol * Thymol * Valerenic Acid (Valerian)
* See here for a full list of GABAA positive allosteric modulators.
Antagonists: Main Site: Bicuculline * Gabazine; Negative Allosteric Modulators: α5IA * Bilobalide * Cicutoxin * DMCM * Flumazenil * Flurothyl * Furosemide * L-655,708 * Oenanthotoxin * Penicillin * Pentylenetetrazol * Picrotoxin * Pitrazepin * PWZ-029 * Ro15-4513 * Sarmazenil * Suritozole * Thujone (Absinthe) * Thiocolchicoside
GABABAgonists: Main Site: 1,4-Butanediol * Baclofen * GBL * GHB * GHV * GVL * Phenibut * Progabide * SKF-97541 * Tolgabide; Positive Allosteric Modulators: BHF-177 * BHFF * BSPP * CGP-7930 * GS-39783
Antagonists: Main Site: CGP-35348 * Phaclofen * Saclofen * SCH-50911
GABACAgonists: Main Site: CACA * CAMP * GABOB * N(4)-chloroacetylcytosine arabinoside * Progabide * Tolgabide
Antagonists: Main Site: Bilobalide * TPMPA
Reuptake
Inhibitors
Receptor
Ligands
GABAAAgonists: Main Site: Bamaluzole * Gaboxadol * Ibotenic Acid * Isoguvacine * Isonipecotic Acid * Muscimol (Amanita Muscaria) * Progabide * SL 75102 * Thiomuscimol * Tolgabide; Positive Allosteric Modulators: Barbiturates * Benzodiazepines * Carbamates * Chlormezanone * Clomethiazole * Etazolate * Ethanol (Alcohol) * Etomidate * Kavalactones (Kava Kava) * Loreclezole * Neuroactive Steroids * Nonbenzodiazepines * Phenols * Piperidinediones * Propanidid * Quinazolinones * ROD-188 * Skullcap * Stiripentol * Thymol * Valerenic Acid (Valerian)
* See here for a full list of GABAA positive allosteric modulators.
Antagonists: Main Site: Bicuculline * Gabazine; Negative Allosteric Modulators: α5IA * Bilobalide * Cicutoxin * DMCM * Flumazenil * Flurothyl * Furosemide * L-655,708 * Oenanthotoxin * Penicillin * Pentylenetetrazol * Picrotoxin * Pitrazepin * PWZ-029 * Ro15-4513 * Sarmazenil * Suritozole * Thujone (Absinthe) * Thiocolchicoside
GABABAgonists: Main Site: 1,4-Butanediol * Baclofen * GBL * GHB * GHV * GVL * Phenibut * Progabide * SKF-97541 * Tolgabide; Positive Allosteric Modulators: BHF-177 * BHFF * BSPP * CGP-7930 * GS-39783
Antagonists: Main Site: CGP-35348 * Phaclofen * Saclofen * SCH-50911
GABACAgonists: Main Site: CACA * CAMP * GABOB * N(4)-chloroacetylcytosine arabinoside * Progabide * Tolgabide
Antagonists: Main Site: Bilobalide * TPMPA
Reuptake
Inhibitors
subgroup |groupstyle=background-color: LightYellow |Plasmalemmal |
GAT InhibitorsCI-966 * Deramciclane * EF-1502 * Gabaculine * Guvacine * Nipecotic acid * NNC 05-2090 * SKF-89976A * SNAP-5114 * Tiagabine
Receptor
Ligands
GABAAAgonists: Main Site: Bamaluzole * Gaboxadol * Ibotenic Acid * Isoguvacine * Isonipecotic Acid * Muscimol (Amanita Muscaria) * Progabide * SL 75102 * Thiomuscimol * Tolgabide; Positive Allosteric Modulators: Barbiturates * Benzodiazepines * Carbamates * Chlormezanone * Clomethiazole * Etazolate * Ethanol (Alcohol) * Etomidate * Kavalactones (Kava Kava) * Loreclezole * Neuroactive Steroids * Nonbenzodiazepines * Phenols * Piperidinediones * Propanidid * Quinazolinones * ROD-188 * Skullcap * Stiripentol * Thymol * Valerenic Acid (Valerian)
* See here for a full list of GABAA positive allosteric modulators.
Antagonists: Main Site: Bicuculline * Gabazine; Negative Allosteric Modulators: α5IA * Bilobalide * Cicutoxin * DMCM * Flumazenil * Flurothyl * Furosemide * L-655,708 * Oenanthotoxin * Penicillin * Pentylenetetrazol * Picrotoxin * Pitrazepin * PWZ-029 * Ro15-4513 * Sarmazenil * Suritozole * Thujone (Absinthe) * Thiocolchicoside
GABABAgonists: Main Site: 1,4-Butanediol * Baclofen * GBL * GHB * GHV * GVL * Phenibut * Progabide * SKF-97541 * Tolgabide; Positive Allosteric Modulators: BHF-177 * BHFF * BSPP * CGP-7930 * GS-39783
Antagonists: Main Site: CGP-35348 * Phaclofen * Saclofen * SCH-50911
GABACAgonists: Main Site: CACA * CAMP * GABOB * N(4)-chloroacetylcytosine arabinoside * Progabide * Tolgabide
Antagonists: Main Site: Bilobalide * TPMPA
Reuptake
Inhibitors
subgroup |groupstyle=background-color: LightYellow |Plasmalemmal |
GAT InhibitorsCI-966 * Deramciclane * EF-1502 * Gabaculine * Guvacine * Nipecotic acid * NNC 05-2090 * SKF-89976A * SNAP-5114 * Tiagabine



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