Tenocyclidine API Manufacturers & Suppliers
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Tenocyclidine | CAS No: 21500-98-1 | GMP-certified suppliers
A medication that is primarily used as a research tool targeting NMDA receptors for neuropharmacological studies related to central nervous system disorders and neuroprotection.
Therapeutic categories
Primary indications
- Because of its high affinity for the phencyclidine binding site on the NMDA receptor, the 3H radiolabelled form of tenocyclidine is widely used in research into NMDA receptors
Product Snapshot
- Tenocyclidine is a small molecule compound primarily used in research applications rather than formulated for clinical administration
- Its main use is as a radiolabelled ligand targeting NMDA receptors in neuropharmacological studies
- The compound is not approved by major regulatory agencies such as FDA or EMA and is considered experimental and investigational
Clinical Overview
Clinically, Tenocyclidine is not approved for medical treatment but serves as a valuable research tool due to its high binding affinity for the phencyclidine site on the NMDA receptor complex. Radiolabeled 3H-Tenocyclidine is frequently employed in neuropharmacological studies exploring NMDA receptor subtypes and their physiological roles.
Pharmacodynamically, Tenocyclidine functions as a non-competitive antagonist at the 3A subunit of the human NMDA receptor (NMDAR), which plays a central role in excitatory neurotransmission and synaptic plasticity. Compared to phencyclidine, TCP demonstrates increased NMDA receptor affinity and reduced sigma receptor binding. Additionally, TCP interacts with the dopamine transporter (DAT) at the D1 subunit, antagonizes the α7-subunit of nicotinic acetylcholine receptors (nAChR), and exhibits binding activity at mu-opioid receptors, suggesting a complex mechanism that may contribute to its neuropharmacological effects and toxicity profile.
Data on absorption, distribution, metabolism, and excretion (ADME) of Tenocyclidine remain limited due to its restricted use. However, its central nervous system potency and receptor profile indicate significant blood-brain barrier penetration and prolonged receptor occupancy. Safety considerations underscore its neurotoxic potential and abuse liability, reflected in its illicit status and absence of therapeutic authorization.
Among known compounds, Tenocyclidine is categorized alongside CNS agents, NMDA receptor antagonists, piperidines, and substances with neuroprotective or neurotoxic potential. It is not marketed under commercial brand names but is recognized in forensic and research contexts.
For API procurement, sourcing Tenocyclidine requires adherence to strict regulatory controls due to its schedule classification and potential misuse. Quality assurance must ensure compliance with international regulations, rigorous purity standards, and secure supply chain management to mitigate risks associated with unauthorized distribution.
Identification & chemistry
| Generic name | Tenocyclidine |
|---|---|
| Molecule type | Small molecule |
| CAS | 21500-98-1 |
| UNII | 8BQ45Q6VCL |
| DrugBank ID | DB01520 |
Pharmacology
| Summary | Tenocyclidine acts primarily as a non-competitive antagonist at the 3A subunit of the NMDA receptor, modulating glutamatergic neurotransmission. It also exhibits activity at the alpha-7 nicotinic acetylcholine receptor, dopamine transporter (DAT), and mu-opioid receptor, contributing to its pharmacodynamic profile. These interactions underpin its utility in research targeting NMDA receptor function and related neural pathways. |
|---|---|
| Mechanism of action | The primary interactions are as a non-competitive antagonist at the 3A-subunit of the NMDAR in Homo sapiens. TCP is known to bind, with relatively high affinity, to the D1 subunit of the human DAT, in addition to displaying a positive antagonistic effect at the α7-subunit of the Nicotinic Acetylcholine Receptor (nAChR). It also binds to the mu-opioid receptor, which seems to be a central part of the mechanism of action of drugs in this class. (For example, Dizocilpine [MK-801] shows little appreciable analgesic effect despite having a high specificity for the NMDA-3A and NMDA-3B subunits - this may well be mediated by the lack of related efficacy at the mu-opioid receptor, though the NMDAR certainly does play a role in transmission of pain signals). |
| Pharmacodynamics | When compared to phencyclidine, tenocyclidine presents more affinity for NMDA receptors and less affinity for sigma receptors. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Glutamate receptor ionotropic, NMDA 3A | Humans | antagonist |
| Glutamate receptor ionotropic, NMDA 3B | Humans | antagonist |
| Glutamate receptor ionotropic, NMDA 2A | Humans | antagonist |
Formulation & handling
- Tenocyclidine is a small molecule with low aqueous solubility, which may require formulation strategies to enhance bioavailability for oral administration.
- Due to its high LogP value, consideration should be given to lipid-based formulations or solubilizing excipients to improve dissolution.
- Handling should account for its investigational and illicit classification, ensuring compliance with regulatory and safety protocols during procurement and formulation.
Regulatory status
Tenocyclidine is a type of Psychopharmaceuticals
Psychopharmaceuticals are a crucial subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that are designed to treat mental health disorders. These medications play a vital role in managing various psychiatric conditions, including depression, anxiety, schizophrenia, bipolar disorder, and attention-deficit/hyperactivity disorder (ADHD).
Psychopharmaceutical APIs act on the central nervous system (CNS) to alter brain chemistry and neurotransmitter activity. They can modulate the levels of neurotransmitters such as serotonin, dopamine, and norepinephrine, which are involved in regulating mood, cognition, and emotions. By targeting these neurotransmitter systems, psychopharmaceuticals help restore the balance of chemicals in the brain, alleviating symptoms and improving overall mental well-being.
These APIs are developed through rigorous research and development processes, involving extensive clinical trials to ensure their safety and efficacy. Manufacturers adhere to stringent quality standards and regulations to produce psychopharmaceutical APIs that meet the highest pharmaceutical industry standards.
The production of psychopharmaceutical APIs requires advanced technologies and specialized equipment to achieve precise control over the manufacturing process. This ensures the consistency and purity of the APIs, which is crucial for producing reliable and effective psychopharmaceutical formulations.
The market for psychopharmaceuticals is growing rapidly due to increasing awareness and recognition of mental health disorders. With the rising demand, pharmaceutical companies are continuously investing in research and development to discover novel psychopharmaceutical APIs and improve existing formulations.
In conclusion, psychopharmaceutical APIs form a vital subcategory of pharmaceutical ingredients used to treat mental health disorders. These medications act on the central nervous system to modulate neurotransmitter activity and restore the balance of brain chemistry. The development and manufacturing of psychopharmaceutical APIs require advanced technologies and adherence to stringent quality standards. With the growing demand for mental health treatments, the psychopharmaceutical market continues to evolve, offering new therapeutic options for patients in need.
Tenocyclidine (Psychopharmaceuticals), 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.
