New Baclofen 99% CAS 1134-47-0 View larger

Baclofen 99% CAS 1134-47-0

Baclofen as a full agonist at the GABA-B receptor acts as a centrally-acting anxiolytic and skeletal muscle relaxant.  As well, it shows efficacy in treatment of alcohol cessation.  

Research Indications:  GABAergic Research, Anxiolytic Research, Addiction Cessation Research

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Baclofen as a full agonist at the GABA-B receptor acts as a centrally-acting anxiolytic and skeletal muscle relaxant.  As well, it shows efficacy in treatment of alcohol cessation. 

Baclofen is rapidly absorbed after oral administration and is widely distributed throughout the body. Biotransformation is low and the drug is predominantly excreted unchanged by the kidneys.The half life of baclofen is roughly 2–4 hours and it therefore needs to be administered frequently for a continual blood level active.

Synonym: 4-Amino-3-(4-chlorophenyl)butanoic acid; Lioresal; (± )-beta-(Aminomethyl)-4-chlorobenzenepropanoic acid
Application: A selective agonist of the GABAB receptor
CAS Number: 1134-47-0
Purity: 99%
Molecular Weight: 213.66
Molecular Formula: C10H12ClNO2

IC50: GABA-B receptor 2: IC50 = 35 nM (human); GABA-B receptor 2: IC50 = 60 nM (rat); GABA-A receptor; anion channel: IC50 = 30 nM (rat)
Ki Data: Displacement of [3H]GABA from GABAB receptor: Ki= 220 nM (rat brain synaptic membranes)
pK Values: pKa: 4, pKb: 10.33 (Predicted)

Solublilty: Soluble in water (pH 7.6) (4.3 mg/ml), dilute aqueous acid (> 20 mg/ml), dilute aqueous base (>20 mg/ml), ethanol (0.02 mg/ml), and methanol (slightly soluble). Insoluble in acetone, chloroform, and ether.

The Many Benefits of Baclofen: A Scientific Review Article

Though baclofen isn't exactly a 'new' drug - it is a very effective medication that is often overlooked. The chemical has incredibly unique properties, and unlike GABA-A selective agonists, it can actually increase/potentiate dopamine release(1). Acknowledging the striatal occupancy of baclofen and the enduring dopaminergic effects(2)(3) has led to the proposal of it's use in cocaine addiction as an anti-craving medication(4) as well as a utility in opioid and alcohol dependence(5)(6)(7). It also runs a lower risk of dependency than benzo's, and withdrawal, though a possibility, is on average less frequent than benzo's - and usually not a concern in short-term (acute) therapeutic use of the drug(8)(9).

aclofen has significant anxiolytic properties; that is it alleviates anxiety - and it seems to be applicable in a wide array of stress related conditions such as:

  • PTSD(10),

  • Alcoholism & Withdrawal(11),

    Repeated Social Stress(12).


    Additionally, baclofen has been shown to decrease serotonin release in the gut(13), as opposed benzo's and selectice GABA-A agonists which may increase it. The implications of this are that baclofen may have the ability to affect the outcome of irritable bowel syndrome and may decrease the incidence of diarrhea and abdominal pain(14)(15). Although not strictly by a serotonergic mechanism, baclofen has shown current use in the treatment of spastic colon (IBS) as evidenced by positive experiences and treatment outcomes. 
    Additionally, baclofen is often prescribed as part of a regimen to counteract Gastro-Oesophageal-Reflux-Disease (G.E.R.D) and is shown to be quite effective(16)(17).

    So baclofen is not your typical muscle relaxant, as it seems to have these effects inward as well. With anti-contractile effects in the gut and in regards to neurons secreting PH efflux toward the esophagus, baclofen is effective. These all point to a very diverse substance with minimal peripheral / systemic side-effects. The additional uses with regard to psychosomatic worries and stimulant dependence also seem to be quite promising


A scientific Utility unveiling the Biological Relevance & Differentiation of GABA-B Receptors

Baclofen is also an efficient tool in scientific study and has nearly made a revolution in terms of actively demonstrating the function of the GABA-B receptor with relation to behavioral, neurological and adrenal role's(22)(23)(24). Due to specific studies involving hypothalamic slices/cultures (in vitro) - we now can characterize and differentiate the roles of each GABA receptor, helping us to understand more the specific inhibitory and / or stimulatory actions of the pathway(25).

The endocrine actions of Baclofen reveal a site-interaction and modulation between GABA-B receptor complex and opioid-receptor signaling
(26)(27). Baclofen is demonstrated to yield robust reductions in cortisol secretion during hypoglycemia and in response to stress(28).

This may underlie the potential for it in managing blood sugar and delaying onset of diabetes shown in 
this study.


Restless Legs Syndrome is a common
 complaint in the USA, and baclofen seems to be one of the most efficacious treatments next to dopaminergic drugs and GABApentin(29)(30).

Baclofen's steady use is most associated with tension in sports injuries and in some autoimmune disorders, and it is also widely studied in spinal cord injuries(31)(32)(33)

Intrathecal Baclofen administration is a common course of action in MS patients and is well-tolerated . The attenuation of spasticity in MS patients with baclofen is remarkable and the low-side-effect profile contributes to the overall appeal in MS with the drug(34)(35).

baclofen has been found to remedy and attenuate some side-effects associated with anti-psychotic drugs, notably the akathisia (Inner Restlessness) and muscular restlessness(36)(37)(38).

Finally, baclofen is a distinct Anti-HICCUP agent, and as such may be a most valuable lesson in the neuro-physiology of muscular function relating to the digestive system. Because baclofen effectively alleviates hiccups of idiopathic origin, this has long-standing implications in how we go about medicating those patients who present with both gastrointestinal and muscular complaints

In conclusion, Baclofen is useful and has shown efficacy for the following .

  • Spasticity in Multiple Sclerosis.

  • Restless Legs Syndrome.

  • Muscle Tension after Spinal Injury.

  • G.E.R.D Complaints.

  • Hiccups.

  • Some features of I.B.S; diarrhea.

  • PTSD and chronic Stress.

  • Anxiety**

  • Alcoholism, Stimulant Dependence and Reducing Cocaine Cravings.

  • Alleviation of Anti-Psychotic Induced Akathisia.**

** = some evidence, better results when co-administered with another drug or as an augmentive therapy. May not apply to all cases.

USAGE: For Research Use Only! Not For Use in Humans.