Muscle relaxant action of MS-322, a new centrally acting muscle relaxant, in rats. 1998

T Otsu, and T Nagao, and H Ono
Department of Toxicology and Pharmacology, Faculty of Pharmaceutical Sciences, University of Tokyo, Japan.

1. The pharmacological properties of (R)-(+)-3-phenyl-5-¿2-(1-pyrrolidinylmethyl)-butyryl¿isoxazole hydrochloride (MS-322) were investigated and compared with those of other muscle relaxants. 2. MS-322 (3-12 mg/kg, IV) reduced spinal reflex potentials in acutely spinalized rats dose dependently. Its inhibitory effects on polysynaptic and dorsal root reflexes were more marked than those on the monosynaptic reflex. 3. MS-322 (1.5-12.0 mg/kg, IV) depressed the afferent discharges of de-efferented muscle spindles in anesthetized rats dose dependently. 4. The inhibitory effect of MS-322 on this afferent activity was considered to be due to its membrane stabilizing action. 5. In addition to the central effects of MS-322, its effect on muscle spindles may contribute to its muscle relaxant activity.

UI MeSH Term Description Entries
D007555 Isoxazoles Azoles with an OXYGEN and a NITROGEN next to each other at the 1,2 positions, in contrast to OXAZOLES that have nitrogens at the 1,3 positions. Isoxazole
D008297 Male Males
D009046 Motor Neurons Neurons which activate MUSCLE CELLS. Neurons, Motor,Alpha Motorneurons,Motoneurons,Motor Neurons, Alpha,Neurons, Alpha Motor,Alpha Motor Neuron,Alpha Motor Neurons,Alpha Motorneuron,Motoneuron,Motor Neuron,Motor Neuron, Alpha,Motorneuron, Alpha,Motorneurons, Alpha,Neuron, Alpha Motor,Neuron, Motor
D009125 Muscle Relaxants, Central A heterogeneous group of drugs used to produce muscle relaxation, excepting the neuromuscular blocking agents. They have their primary clinical and therapeutic uses in the treatment of muscle spasm and immobility associated with strains, sprains, and injuries of the back and, to a lesser degree, injuries to the neck. They have been used also for the treatment of a variety of clinical conditions that have in common only the presence of skeletal muscle hyperactivity, for example, the muscle spasms that can occur in MULTIPLE SCLEROSIS. (From Smith and Reynard, Textbook of Pharmacology, 1991, p358) Centrally Acting Muscle Relaxants,Central Muscle Relaxants,Relaxants, Central Muscle
D009126 Muscle Relaxation That phase of a muscle twitch during which a muscle returns to a resting position. Muscle Relaxations,Relaxation, Muscle,Relaxations, Muscle
D009475 Neurons, Afferent Neurons which conduct NERVE IMPULSES to the CENTRAL NERVOUS SYSTEM. Afferent Neurons,Afferent Neuron,Neuron, Afferent
D011759 Pyrrolidines Compounds also known as tetrahydropyridines with general molecular formula (CH2)4NH. Tetrahydropyridine,Tetrahydropyridines
D012018 Reflex An involuntary movement or exercise of function in a part, excited in response to a stimulus applied to the periphery and transmitted to the brain or spinal cord.
D003655 Decerebrate State A condition characterized by abnormal posturing of the limbs that is associated with injury to the brainstem. This may occur as a clinical manifestation or induced experimentally in animals. The extensor reflexes are exaggerated leading to rigid extension of the limbs accompanied by hyperreflexia and opisthotonus. This condition is usually caused by lesions which occur in the region of the brainstem that lies between the red nuclei and the vestibular nuclei. In contrast, decorticate rigidity is characterized by flexion of the elbows and wrists with extension of the legs and feet. The causative lesion for this condition is located above the red nuclei and usually consists of diffuse cerebral damage. (From Adams et al., Principles of Neurology, 6th ed, p358) Decerebrate Posturing,Decorticate Rigidity,Decorticate State,Rigidity, Decerebrate,Rigidity, Decorticate,Decerebrate Posturings,Decerebrate Rigidity,Decerebrate States,Decorticate Rigidities,Decorticate States,Posturing, Decerebrate,Posturings, Decerebrate,Rigidities, Decorticate,State, Decerebrate,States, Decerebrate
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia

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