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Cyclobenzaprine-d6 is intended for use as an internal standard for the quantification of cyclobenzaprine by GC- or LC-MS. Cyclobenzaprine is a skeletal muscle relaxant.1,2,3 It is an antagonist of M1, M2, and M3 muscarinic acetylcholine receptors (mAChRs; Kis = 25, 60, and 6 nM, respectively), the histamine H1 receptor (IC50 = 20 nM), and serotonin (5-HT) receptor subtypes 5-HT2A, 5-HT2B, and 5-HT2C (Kis = 1,685, 330, and 56 nM, respectively). Cyclobenzaprine (1 mg/kg) prevents increases in the flexor reflex induced by the 5-HT2 receptor agonist DOI in spinalized rats.3 Formulations containing cyclobenzaprine have been used as muscle relaxants.
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1. Identifying mechanism-
2. Large scale prediction and testing of drug activity on side-
3. Tricyclic analogs cyclobenzaprine, amitriptyline and cyproheptadine inhibit the spinal reflex transmission through 5-