Effects of NK433, a new centrally acting muscle relaxant, on masticatory muscle reflexes in rats.
The effects of (-)-(R)-2-methyl-3-(1-pyrrolidinyl)-4'- trifluoromethylpropiophenone monohydrochloride (NK433), a novel centrally acting muscle relaxant, on masticatory muscle reflexes were investigated in rats. NK433 inhibited the monosynaptic tonic vibration reflex of the masseter muscle and the polysynaptic tonic periodontal masseteric reflex. These reflexes are increased by gamma-motor activity. NK433 had a weak inhibitory effect on the polysynaptic jaw opening reflex evoked by electrical stimulation of the tooth pulp, which is little related with gamma-motor activity. Eperisone-HCl depressed the three types of masticatory muscle reflexes. When intravenously administered, eperisone-HCl was equipotent to NK433, but the effect of eperisone-HCl was shorter-lasting than that of NK433. The effect of intragastrically administered NK433 on the periodontal masseteric reflex was about three times stronger than that of eperisone-HCl. These results suggest that NK433 inhibits masticatory muscle reflexes controlled by the gamma-motor system and thus may ameliorate the temporomandibular joint syndrome in man.
Ozawa
Y
Y
Research & Development Division, Nippon Kayaku Co. Ltd., Tokyo, Japan.
Komai
C
C
Sakitama
K
K
Ishikawa
M
M
D000818:Animals; D004305:Dose-Response Relationship, Drug; D008297:Male; D008410:Masticatory Muscles / Q000187:drug effects* / Q000502:physiology; D009125:Muscle Relaxants, Central / Q000494:pharmacology*; D011427:Propiophenones / Q000494:pharmacology*; D011759:Pyrrolidines / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D012018:Reflex / Q000187:drug effects*
D009125:Muscle Relaxants, Central; D011427:Propiophenones; D011759:Pyrrolidines; C030848:eperisone; C093390:NK 433