CS 722 - CAS 144886-17-9
Catalog number: 144886-17-9
Category: Inhibitor
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CS 722 is a neuromuscular blocking agent and centrally acting muscle relaxant. It exerts its muscle relaxant action by affecting both the supraspinal structure and the spinal cord. In Oct 2000, Phase II for Hypertonia in Japan was discontinued.
CS 722; CS-722; CS722. 4-Chloro-2-(2-hydroxy-3-morpholinopropyl)-5-phenyl-4-isoxazolin-3-one
Soluble in DMSO
-20°C Freezer
Muscle hypertonia
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
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Current Developer:
Originator Sankyo
1.Mechanisms of spinal reflex depressant effects of CS-722, a newly synthesized centrally acting muscle relaxant, in spinal rats.
Tanabe M;Kaneko T;Tonohiro T;Iwata N Neuropharmacology. 1992 Sep;31(9):949-54.
The mechanisms of the depressant action of (R)-4-chloro-2-(2-hydroxy-3-morpholinopropyl)-5-phenyl-4-isoxaz olin-3-one hydrochloride (CS-722), a newly synthesized centrally acting muscle relaxant, on spinal reflexes were investigated in spinal rats. The drug CS-722 (50 mg/kg, i.v.) depressed the polysynaptic reflex but was less effective on the monosynaptic reflex. Eperisone-HCl (10 mg/kg, i.v.) and baclofen (2 mg/kg, i.v.) markedly decreased the monosynaptic and polysynaptic reflexes, with longer durations than CS-722; CS-722, eperisone and baclofen depressed the dorsal root reflex. The excitability of the motoneurone was reduced by CS-722 and eperisone. Excitability of the primary afferent fibres was reduced by CS-722, while eperisone and baclofen had no effect. Both CS-722 and eperisone did not have a depressant influence on the focal synaptic potential. These results suggest that CS-722 and eperisone but not baclofen, have a common motoneurone-membrane-stabilizing action and that this action may contribute, in part, to the spinal reflex depressant effects of CS-722 and eperisone.
2.The pharmacological properties of CS-722, a newly synthesized centrally acting muscle relaxant.
Tanabe M;Kaneko T;Tonohiro T;Iwata N Neuropharmacology. 1992 Oct;31(10):1059-66.
The pharmacological properties of (R)-4-chloro-2-(2-hydroxy-3-morpholinopropyl)-5-phenyl-4-isoxaz olin-3-one hydrochloride (CS-722), a newly synthesized, centrally acting muscle relaxant, were studied in rats. The drug CS-722 reduced the radio frequency decerebrate rigidity in a dose-dependent manner (25-100 mg/kg, p.o.); it inhibited the increase in discharges from Ia afferent fibers, gamma-motor activity, which was induced by stimulation of the reticular formation. The compound, however, showed no effect on the basal discharge of Ia afferent fibers. The polysynaptic reflex was depressed by CS-722, with less influence on the monosynaptic reflex in intact and spinal preparations and CS-722 did not prolong thiopental-induced sleeping time. In rats anesthetized with halothane, CS-722 did not affect the electroencephalogram (EEG) arousal response, which was elicited by stimulation of the reticular formation. The results of this study suggest that CS-722 can exert a muscle relaxant action, at a dose range at which depression of the ascending reticular activating system was negligible. The results also suggest that depressions of the gamma-motor system and the polysynaptic reflex may contribute to the muscle relaxant action of CS-722.
3.The effects of the muscle relaxant, CS-722, on synaptic activity of cultured neurones.
Marszalec W;Song JH;Narahashi T Br J Pharmacol. 1996 Sep;119(1):126-32.
1. The pharmacological properties of the centrally acting muscle relaxant, CS-722, were studied in cultured hippocampal cells and dorsal root ganglion cells of the rat using the whole-cell variation of the patch clamp technique. 2. CS-722 inhibited the occurrence of spontaneous excitatory and inhibitory postsynaptic currents in hippocampal neurones at concentrations of 100-300 microM, but had no effect on postsynaptic currents evoked by the application of glycine, gamma-aminobutyric acid, glutamate or N-methyl-D-aspartate. 3. CS-722 reduced voltage-gated sodium currents, while shifting the sodium channel inactivation curve to more negative membrane potentials. This effect is similar to that reported for local anaesthetics. Voltage-gated potassium currents were decreased by CS-722 by approximately 20%, whereas voltage-activated calcium currents were inhibited by about 25%. 4. CS-722 inhibited evoked inhibitory postsynaptic currents. However, the spontaneous quantal release of inhibitory transmitter was not affected. 5. The inhibitory effect of CS-722 on spontaneous inhibitory postsynaptic currents and excitatory postsynaptic currents in hippocampal cultures probably results from an inhibition of both sodium and calcium currents.
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CAS 144886-17-9 CS 722

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