| Bioactivity | Cyclobenzaprine hydrochloride (MK130 hydrochloride) is a skeletal muscle relaxant and a central nervous system (CNS) depressant.Target: 5-HT Receptor 2ACyclobenzaprine hydrochloride is a skeletal muscle relaxant and a central nervous system (CNS) depressant. Cyclobenzaprine hydrochloride was thought to be an alpha 2-adrenoceptor agonist that reduced muscle tone by decreasing the activity of descending noradrenergic neurons. Cyclobenzaprine hydrochloride reduced the monosynaptic reflex amplitude dose dependently and this effect was not inhibited by the alpha 2-adrenoceptor antagonists idazoxan and yohimbine. Cyclobenzaprine-induced monosynaptic reflex depression was not attenuated by noradrenergic neuronal lesions produced by 6-hydroxydopamine. Cyclobenzaprine hydrochloride is a 5-HT2 receptor antagonist and that its muscle relaxant effect is due to inhibition of serotonergic, not noradrenergic, descending systems in the spinal cord [1]. The inhibitory effects of Cyclobenzaprine hydrochloride on mono- and polysynaptic reflex potentials are due to the inhibition of descending serotonergic systems through 5-HT(2) receptors in the spinal cord [2]. |
| Name | Cyclobenzaprine hydrochloride |
| CAS | 6202-23-9 |
| Formula | C20H22ClN |
| Molar Mass | 311.85 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [1]. Kobayashi, H., Y. Hasegawa, and H. Ono, Cyclobenzaprine, a centrally acting muscle relaxant, acts on descending serotonergic systems. Eur J Pharmacol, 1996. 311(1): p. 29-35. [2]. Honda, M., T. Nishida, and H. Ono, Tricyclic analogs cyclobenzaprine, amitriptyline and cyproheptadine inhibit the spinal reflex transmission through 5-HT(2) receptors. Eur J Pharmacol, 2003. 458(1-2): p. 91-9. |