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Pidolic acid API Manufacturers & Suppliers

General Description:

Pidolic acid, identified by CAS number 98-79-3, is a notable compound with significant therapeutic applications. Pidolic acid is a naturally occurring but little-studied amino acid derivative that can be formed enzymatically or non-enzymatically and participates as a biological intermediate with unique pharmacodynamics in various chemical pathways . Elevations of the acid in blood levels may be associated with problems of glutamine or glutathione metabolism . Pidolic acid, in general, is found in large quantities in brain tissue and other tissues in bound form, like skin . There are currently little to no medicines available that are clinically approved or marketed for employing pidolic acid as an active ingredient for any particular formal indication. Although pidolic acid is included in some over-the-counter, non-prescription dietary supplements for the proposed purpose of facilitating cognitive or memory enhancement, most available research suggest exercising caution in their recommendation as much more research is necessary .

Indications:

This drug is primarily indicated for: There is currently no clinically approved and/or marketed medicine that relies upon pidolic acid as an active ingredient for any formal therapeutic indication. Although pidolic acid may be sold in a variety of non-prescription, over-the-counter dietary supplement products for cognitive or memory enhancement, there are many studies that suggest that such products or such supplementation do not elicit any kind of cognitive benefit to users . In fact, the general suggestion for any such pidolic acid product is to exercise caution in their recommendation as much more research is necessary . Pidolic acid and sodium pidolic acid are, however, used to some extent in skin and hair conditioning agents owing to their humectant characteristics . Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

Pidolic acid undergoes metabolic processing primarily in: In living cells, various metabolic pathways involving pidolic acid exist: (a) glutamyl/glutaminyl (amino acid) n is converted to pyroglutamyl- (amino acid) n by glutaminyl cyclase, pyroglutamyl- (amino acid) n is then metabolised to pyroglutamic acid (pidolic acid) by pyroglutamyl peptidase; (b) via the gamma-Glutamyl cycle, gamma-Glutamyl transpeptidase generates gamma-Glutamyl amino acid which is metabolised to pyroglutamic acid via gamma-Glutamyl cyclotransferase; (c) glutamate via gamma-Glutamylcysteine synthetase or Glutamine synthetase or Glutamate 5-kinase metabolism generates gamma-Glutamyl phosphate which itself can be converted to pyroglutamic acid; and (d) glutamate or glutamine can be non-enzymatically converted to pyroglutamic acid . Finally, pyroglutamic acid (or pidolic acid) itself is metabolized to glutamate via the 5-Oxoprolinase enzyme . This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Absorption:

The absorption characteristics of Pidolic acid are crucial for its therapeutic efficacy: In skin conditioning agents, it has been observed that the percutaneous absorption of 5, 10, and 20% sodium pidolic acid through human skin was 5.97, 6.78, and 5.89%, respectively . The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Half-life:

The half-life of Pidolic acid is an important consideration for its dosing schedule: Some studies have determined that the specific half-life of the N-terminal glutamic acid is about 9 months in a pH 4.1 buffer at 45 degrees Celsius . This determines the duration of action and helps in formulating effective dosing regimens.

Protein Binding:

Pidolic acid exhibits a strong affinity for binding with plasma proteins: Readily available data regarding the protein binding of pidolic acid is not available. This property plays a key role in the drug's pharmacokinetics and distribution within the body.

Route of Elimination:

The elimination of Pidolic acid from the body primarily occurs through: In the dog animal model, it was determined that 30% of an absorbed oral administration of pidolic acid was excreted unchanged in the urine and the remainder converted to urea . Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Volume of Distribution:

Pidolic acid is distributed throughout the body with a volume of distribution of: Readily available data regarding the volume of distribution of pidolic acid is not available. This metric indicates how extensively the drug permeates into body tissues.

Clearance:

The clearance rate of Pidolic acid is a critical factor in determining its safe and effective dosage: Readily available data regarding the clearance of pidolic acid is not available. It reflects the efficiency with which the drug is removed from the systemic circulation.

Pharmacodynamics:

Pidolic acid exerts its therapeutic effects through: Pidolic acid is a naturally occurring but little-studied amino acid derivative that can be formed enzymatically or non-enzymatically and participates as a biological intermediate in various chemical pathways . Elevations of the acid in blood levels may be associated with problems of glutamine or glutathione metabolism . Pidolic acid, in general, is found in large quantities in brain tissue and other tissues in bound form, like skin . Moreover, pidolic acid in high enough levels can act as an acidogen capable of inducing acidosis and a metabotoxin that can result in adverse health effects . Chronically elevated levels of pidolic acid are associated with at least five inborn errors of metabolism including 5-oxoprolinuria (where 5-oxoproline is otherwise known as pidolic acid), 5-oxoprolinase deficiency, glutathione synthetase deficiency, hawkinsinuria, and propionic acidemia . In particular, abnormally high levels of organic acids like pidolic acid in the blood, urine, brain, and/or other tissues results in general metabolic acidosis . Such acidosis generally occurs when arterial pH falls below 7.35 . In infants, the initial symptoms of acidosis consist of poor feeding, vomiting, loss of appetite, weak muscle tone (hypotonia), and lack of energy . Eventually, acidosis and the symptoms of acidosis can lead to heart, liver, and kidney abnormalities, seizures, coma, and possibly even death . Many children who are afflicted with organic acidemias experience intellectual disability or delayed development. In adults, acidosis or acidemia is characterized by headaches, confusion, feeling tired, tremors, sleepiness, and seizures . High levels of pidolic acid in the blood have also been demonstrated following acetaminophen overdose, causing an increased level of acidity called a high anion gap metabolic acidosis . The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Pidolic acid functions by: Pidolic acid is an endogenous amino acid derivative where the free amino group of glutamic acid or glutamine cyclizes to generate a lactam . Subsequently it is also a metabolite in the glutathione cycle that is converted to glutamate by the enzyme 5-oxoprolinase . Moreover, N-terminal glutamic acid and glutamine residues can either spontaneously cyclize to become pidolic acid, or be enzymatically transformed by glutaminyl cyclases . In particular, this is ultimately a form of N-termini that is a challenge for N-terminal sequencing using Edman chemistry, which necessitates a free primary amino group that is not present in pidolic acid . Pyroglutamate aminopeptidase can restore a free N-terminus by cleaving off the pyroglutamate residue, however . Additionally, pidolic acid and certain pidolic acid salts like calcium, magnesium, and potassium pidolic acid are sometimes used as skin or hair conditioning agents because of their humectant effects . In such humectant formulations, hydrophilic amine, hydroxyl, or even carboxyl groups possess high affinities for forming hydrogen bonds with molecules of water, allowing the hygroscopic formulations to attract and retain moisture in the air nearby through absorption, therefore drawing the water vapor into the formulation. This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Classification:

Pidolic acid belongs to the class of organic compounds known as alpha amino acids and derivatives. These are amino acids in which the amino group is attached to the carbon atom immediately adjacent to the carboxylate group (alpha carbon), or a derivative thereof, classified under the direct parent group Alpha amino acids and derivatives. This compound is a part of the Organic compounds, falling under the Organic acids and derivatives superclass, and categorized within the Carboxylic acids and derivatives class, specifically within the Amino acids, peptides, and analogues subclass.

Categories:

Pidolic acid is categorized under the following therapeutic classes: Alimentary Tract and Metabolism, Amino Acids, Amino Acids, Acidic, Amino Acids, Cyclic, Amino Acids, Peptides, and Proteins, Glutamates, Imino Acids, Mineral Supplements, Pyrrolidines, Pyrrolidinones. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.

Experimental Properties:

Further physical and chemical characteristics of Pidolic acid include:

• Water Solubility: 4.76E+005 mg/L (at 13 °C)
• Melting Point: 184.7 °C