Cabergoline

Price range: $73.00 through $140.00

Chemical Information and Compositions of Cabergoline

For researchers, biochemists, and wholesale distributors, the molecular structure of cabergoline is a masterclass in targeted receptor selectivity and metabolic stability. Understanding its composition is vital for analytical testing, formulation, and predicting its biological behavior.

Official Chemical Nomenclature

  • Chemical Name: (8R)-N-[(3-dimethylamino)propyl]-N-[(ethylcarbamoyl)methyl]-10-methoxy-6-methylergoline-8-carboxamide
  • Chemical Formula: C26H29N5O2
  • Molecular Weight: 451.60 g/mol
  • CAS Number: 81409-02-5

Structural Composition Breakdown

cabergoline is a semi-synthetic ergot alkaloid derivative. Its structural architecture is what gives it its phenomenal D2 selectivity and ultra-long half-life:

  1. The Ergoline Ring System: The core of the molecule features the classic tetracyclic ergoline ring system (shared with Bromocriptine and LSD), which is essential for binding to the dopaminergic receptors.
  2. The C-10 Methoxy Group: The presence of a methoxy group (-OCH3) at the 10th carbon position is critical. This electron-donating group fine-tunes the stereochemistry and electron density of the molecule, drastically increasing its affinity for the dopamine D2 receptor while decreasing its affinity for D1 and serotonin receptors, reducing hallucinations and nausea.
  3. The C-8 Carboxamide Side Chain: The highly polar, bulky N-[(3-dimethylamino)propyl]-N-[(ethylcarbamoyl)methyl] carboxamide side chain at the 8th carbon is the defining structural feature of cabergoline. This side chain contributes massively to the molecule’s metabolic stability. It protects the molecule from rapid hepatic first-pass degradation by cytochrome P450 enzymes, which is the primary reason for its 60+ hour half-life.
  4. Stereochemistry: cabergoline has a chiral center at the 8th carbon (8R configuration). Only this specific stereoisomer possesses the desired dopaminergic activity; the 8S enantiomer is largely inert.

Physical and Chemical Properties

  • State at Room Temperature: Solid (Crystalline Powder)
  • Color: White to off-white
  • Solubility: Practically insoluble in water (0.039 mg/mL). Highly soluble in organic solvents such as DMSO, ethanol, methanol, and ethyl acetate. Due to its poor aqueous solubility, it requires specific pharmaceutical excipients for oral bioavailability.
  • Melting Point: Approximately 102°C to 104°C.

Pharmacokinetics

  • Route of Administration: Oral
  • Absorption: Rapidly absorbed from the gastrointestinal tract. Food does not significantly alter the extent of absorption, though taking it with a meal can mitigate initial nausea.
  • Half-Life: The pharmacokinetic profile of cabergoline is defined by its ultra-long terminal elimination half-life, which ranges from 60 to 65 hours (roughly 2.5 to 3 days) in healthy individuals, and can extend up to 100 hours in hyperprolactinemic patients. This allows for convenient twice-weekly (or even once-weekly) dosing.
  • Metabolism: Extensively metabolized in the liver, primarily via hydrolysis of the acylurea bond and N-dealkylation.
  • Excretion: Excreted mainly in the feces (both as unchanged drug and metabolites), with a small fraction (3-6%) excreted in the urine.

Formulation Details: The Pill

When you source wholesale cabergoline, you are dealing with a micro-dose formulation. Standard clinical pills contain 0.5mg of the active API.

Because 0.5mg is an incredibly small mass, it must be geometrically diluted with excipients to create a handleable, uniform pill. Standard excipients include:

  • Lactose Monohydrate: Diluent/filler to add necessary bulk.
  • Microcrystalline Cellulose (MCC): Binder and filler for structural integrity.
  • Croscarmellose Sodium: Super-disintegrant for rapid dissolution.
  • Povidone (PVP): Binder.
  • Magnesium Stearate: Lubricant to prevent sticking during tableting.

For B2B buyers, ensuring the uniform blending of 0.5mg of API within 100-200mg of these excipients is the single greatest manufacturing challenge. Failure results in “hot spots” (pills with 1.5mg) and “dead spots” (pills with 0mg), which are disastrous for endocrine management.

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