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Lisuride | CAS No: 18016-80-3 | GMP-certified suppliers
A medication that manages Parkinson's disease symptoms by modulating dopaminergic and serotonergic pathways to improve motor function and reduce prolactin levels.
Therapeutic categories
Primary indications
- For the management of Parkinson's Disease
Product Snapshot
- Lisuride is an oral small molecule formulation
- It is primarily used for the management of Parkinson's Disease
- Lisuride has both approved and investigational status in key regulatory markets
Clinical Overview
Pharmacodynamically, lisuride functions mainly as a dopamine receptor agonist, exhibiting high affinity for dopamine D2 receptors while potentially acting as an antagonist at dopamine D1 receptors. It also interacts with several serotonin receptors, notably agonizing 5-HT1A and 5-HT2A/2C subtypes. In addition, lisuride binds to histamine H1 receptors, which may contribute to its overall pharmacological profile. The compound has demonstrated the ability to lower prolactin levels, reflecting its dopaminergic activity.
The mechanism of action involves modulation of central dopaminergic and serotonergic pathways, integral to its therapeutic effects in Parkinson's disease. By stimulating dopamine receptors, lisuride helps mitigate motor symptoms associated with dopamine deficiency. Its serotonergic and histaminergic receptor activity may variably influence efficacy and tolerability.
Lisuride undergoes hepatic metabolism primarily via cytochrome P450 enzymes, including CYP2D6 and CYP3A4 isoforms. Its metabolic profile necessitates careful consideration of drug-drug interactions, especially with agents metabolized by these pathways. Pharmacokinetic data such as absorption, distribution, and elimination rates require context-specific evaluation.
From a safety perspective, lisuride's adverse event profile includes potential central nervous system effects and cardiovascular events linked to its vasoconstrictive ergot structure. Monitoring is advised to mitigate risks of hypertension and serotonergic syndrome when combined with other serotonergic agents. As with other dopamine agonists, impulse control disorders and psychiatric symptoms may occur.
Notable branded formulations of lisuride exist primarily in select markets, and its clinical use can vary based on regional regulatory approvals. It remains an established option within the repertoire of anti-Parkinson drugs, complementing other dopamine agonists and levodopa-based therapies.
For API procurement, sourcing should prioritize rigorous quality control to ensure chemical purity and compliance with pharmacopoeial standards given the complexity of ergot derivatives. Stability, impurity profiles, and consistent batch-to-batch reproducibility are critical parameters. Collaboration with suppliers experienced in handling ergot alkaloids and evidence of suitable Good Manufacturing Practice (GMP) certification is recommended to support formulation and regulatory needs.
Identification & chemistry
| Generic name | Lisuride |
|---|---|
| Molecule type | Small molecule |
| CAS | 18016-80-3 |
| UNII | E0QN3D755O |
| DrugBank ID | DB00589 |
Pharmacology
| Summary | Lisuride is a dopamine receptor agonist with affinity for multiple dopamine receptor subtypes (D1-D5) and serotonin receptors (5-HT1A, 5-HT2A/2C). Its pharmacological activity includes modulation of dopaminergic and serotonergic signaling pathways, contributing to its therapeutic effects in Parkinson's disease and prolactin regulation. Additional receptor interactions include histamine H1 and alpha-2 adrenergic receptors. |
|---|---|
| Mechanism of action | Lisuride is an anti-Parkinson drug chemically related to the dopaminergic ergoline Parkinson's drugs. Lisuride binds to the 5-HT(1A) and 5-HT(2A/2C) receptors. It is also thought to bind to the dopamine receptor and to act as a dopamine agonist. Evidence has also emerged that Lisuride also binds to the Histamine H1 receptor. |
| Pharmacodynamics | There is evidence that lisuride lowers prolactin levels and, in low doses, prevents migraine attacks. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Dopamine D2 receptor | Humans | agonist |
| Dopamine D3 receptor | Humans | agonist |
| Dopamine D4 receptor | Humans | agonist |
ADME / PK
| Protein binding | about 15% |
|---|
Formulation & handling
- Lisuride is a small molecule with moderate lipophilicity suitable for oral formulation development.
- Low aqueous solubility may require formulation strategies to enhance bioavailability.
- As a stable solid with no peptide structure, standard handling and storage conditions are generally adequate.
Regulatory status
Lisuride is a type of Dopamine agonists
Dopamine agonists are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that act on the dopamine receptors in the brain. These compounds mimic the effects of dopamine, a neurotransmitter involved in various physiological processes such as movement, cognition, and emotions.
Dopamine agonists are commonly used in the treatment of neurological disorders, particularly Parkinson's disease and restless legs syndrome. They work by binding to dopamine receptors and stimulating them, thereby increasing dopamine activity in the brain. This helps to alleviate the symptoms associated with these conditions, such as tremors, rigidity, and muscle stiffness.
One of the key advantages of dopamine agonists is their ability to provide long-lasting relief compared to other medications. They are available in different formulations, including oral tablets, transdermal patches, and injectable solutions, allowing patients to choose the most suitable administration method.
However, like any medication, dopamine agonists may have side effects. These can include nausea, dizziness, hallucinations, and compulsive behaviors. It is important for healthcare professionals to closely monitor patients using dopamine agonists to minimize the occurrence and severity of these side effects.
In conclusion, dopamine agonists are a vital subcategory of pharmaceutical APIs used to manage Parkinson's disease and restless legs syndrome. They mimic the effects of dopamine in the brain and offer long-lasting relief from symptoms. Although they can have side effects, proper monitoring and dosage adjustments can help optimize their therapeutic benefits.
Lisuride (Dopamine agonists), classified under Central Nervous System Agents
Central Nervous System (CNS) Agents are a crucial category of pharmaceutical Active Pharmaceutical Ingredients (APIs) that specifically target the central nervous system. The CNS encompasses the brain and spinal cord, playing a vital role in regulating and controlling various bodily functions, including cognition, movement, emotions, and sensory perception. These agents are designed to interact with specific receptors, enzymes, or ion channels within the CNS to modulate neural activity and restore normal functioning.
CNS agents comprise a diverse range of pharmaceutical APIs, including analgesics, anesthetics, antipsychotics, sedatives, hypnotics, anti-epileptics, and antidepressants. Each subcategory addresses distinct neurological disorders and conditions. For instance, analgesics alleviate pain by targeting receptors in the brain and spinal cord, while antipsychotics are employed to manage psychosis symptoms in mental illnesses such as schizophrenia.
The development of CNS agents involves rigorous research, molecular modeling, and extensive clinical trials to ensure safety, efficacy, and specific target engagement. Pharmaceutical companies invest significant resources in identifying novel drug targets, synthesizing new compounds, and optimizing their pharmacological properties. These agents undergo rigorous regulatory evaluations and must adhere to stringent quality standards and guidelines.
Given the prevalence of CNS disorders globally, the market demand for effective CNS agents is substantial. The development of innovative CNS APIs not only improves patient outcomes but also provides valuable commercial opportunities for pharmaceutical companies. Continued advancements in CNS agent research and development hold the promise of groundbreaking therapies that can improve the quality of life for individuals affected by neurological conditions.
Lisuride API manufacturers & distributors
Compare qualified Lisuride API suppliers worldwide. We currently have 1 companies offering Lisuride API, with manufacturing taking place in 1 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| LGM Pharma | Distributor | United States | World | BSE/TSE, CEP, CoA, GMP, MSDS, USDMF | 441 products |
When sending a request, specify which Lisuride API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
Use the list above to find high-quality Lisuride API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
