Ligand id: 7152

Name: cyclobenzaprine

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View more information in the IUPHAR Pharmacology Education Project: cyclobenzaprine

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 1
Hydrogen bond donors 0
Rotatable bonds 3
Topological polar surface area 3.24
Molecular weight 275.17
XLogP 8.49
No. Lipinski's rules broken 1

Molecular properties generated using the CDK

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 III clinical trials as a therepy for fibromyalgia (June 2015), a common, diffucult to treat chronic pain condition. An additional Phase III trial is recruiting patients with various muscular, neuromuscular, nervous system and rheumatic diseases (NCT02436096). A Phase II 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.
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