Synonyms: Amrix® | Fexmid | MK-130
cyclobenzaprine is an approved drug (FDA (1977))
Compound class:
Synthetic organic
Comment: Cyclobenzaprine is a tricyclic antidepressant similar to amitriptyline. It acts as a skeletal muscle relaxant and central nervous system (CNS) depressant.
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖View more information in the IUPHAR Pharmacology Education Project: cyclobenzaprine |
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No information available. |
Summary of Clinical Use |
This drug is used to relieve muscle spasm associated with acute musculoskeletal pain. A sublingually administered formulation of cyclobenzaprine hydrochloride (TNX-102, PubChem CID 22576) is being evaluated in Phase 2I clinical trials as a therepy for fibromyalgia (June 2015), a common, diffucult to treat chronic pain condition. An additional Phase 2I trial is recruiting patients with various muscular, neuromuscular, nervous system and rheumatic diseases (NCT02436096). A Phase 2 trial in military personnel suffering from post-traumatic stress disorder (PTSD) is also underway (see NCT02277704). |
Mechanism Of Action and Pharmacodynamic Effects |
Cyclobenzaprine antagonises central serotonin 5-HT2A and 5-HT2C receptors. This decreases activity in serotonergic neurones innervating the muscle and results in reduced muscle tone. |
External links |
For extended ADME data see the following: Drugs.com |