Pharmacodynamics of chlorzoxazone in rats.

  title={Pharmacodynamics of chlorzoxazone in rats.},
  author={I Kaneko and Yoshinobu Fukumori and Tomoaki Fukuda and Yoshikazu Takeuchi},
  journal={Journal of pharmaceutical sciences},
  volume={77 5},
Pharmacological effect-time profiles of a centrally acting muscle relaxant, chlorzoxazone, were evaluated by both rotarod and crossed extensor reflex (CER) methods. Drug response was measured by percent change in the remaining time on the rod for the former method and in intensity of isometric contraction of the muscle for the latter method. The drug response was quantitated using the logarithmic-logistic function and then biophase levels were calculated. The results indicated that the maximum… 
Influence of alpha-chloralose on muscle relaxant effect of chlorzoxazone in rats and pharmacodynamic analysis.
Pharmacodynamic analysis offered the results that the dose-normalized biophase levels of CZX were coincident with each other when CZX was given at three different doses under ACH anesthesia at the dose of 80 mg/kg, which implied that pharmacological response intensity was reasonably related to the relative biophases CZX level via Hill's equation.
Relation of disposition kinetics to pharmacological effect of intravenous administration of chlorzoxazone in rats.
The quantitative relationship between a drug disposition and the pharmacological effect was examined in rats using chlorzoxazone, a centrally acting muscle relaxant, as a model drug and it was found that the biophase compartment was identical to the central compartment as long as the first order processes were proceeding.
Effect of alpha-chloralose on disposition and pharmacological action of orally administered chlorzoxazone in rats.
The pharmacodynamic behavior of orally administered chlorzoxazone (CZX) was studied in rats and it was found that CZX obeyed a one-compartment model with first-order absorption, suggesting that the pharmacokinetic and pharmacodynamic concept proposed by Smolen was not applicable to CZX's behavior at such a dose in rats.
Effect of the acute-phase response on the pharmacokinetics of chlorzoxazone and cytochrome P-450 2E1 in vitro activity in rats.
  • K. Rockich, R. Blouin
  • Biology, Medicine
    Drug metabolism and disposition: the biological fate of chemicals
  • 1999
It is demonstrated that LPS administration produced expected reductions in the in vivo intrinsic clearance of CZN, and these changes were highly correlated with in vitro activity studies.
Antiparkinson Drug Benztropine Suppresses Tumor Growth, Circulating Tumor Cells, and Metastasis by Acting on SLC6A3/DAT and Reducing STAT3
The repurposing of benztropine is proposed for anticancer research and therapeutics that can suppress tumor progression, CTC, and metastasis of aggressive cancers by reducing key pro-tumorigenic factors.


Simultaneous modeling of pharmacokinetics and pharmacodynamics: Application to d‐tubocurarine
We propose a model of drug pharmacodynamic response that when integrated with a pharmacokinetic model allows characterization of the temporal aspects of pharmacodynamics as well as the
A pharmacological comparison of therapeutically useful centrally acting skeletal muscle relaxants.
  • A. Roszkowski
  • Biology, Chemistry
    The Journal of pharmacology and experimental therapeutics
  • 1960
Anticonvulsant studies carried out with these drugs indicate that chlorzoxazone possesses potent anti-strychnine activity while having virtually no protective action against pentylenetetrazol and meprobamate, which suggests that chlorZoxazolamine may act principally at spinal levels and meProbamate at supraspinal levels.
Effect of centrally acting muscle relaxants on the morphine-induced Straub tail reaction in mice.
It is suggested that the morphine-induced Straub tail reaction is positively depressed by centrally acting muscle relaxants.
The results suggest that the mode of action of afloqualone is different from the actions of mephenesin, chlormezanone, and diazepam, which showed no influence on the neuro-muscular transmission and inhibited little the muscle spindle discharges.
Pharmacological studies on 6-amino-2-fluoromethyl-3-(O-tolyl)-4(3H)-quinazolinone (afloqualone), a new centrally acting muscle relaxant. (II) Effects on the spinal reflex potential and the rigidity.
Afloqualone, like other well known centrally acting muscle relaxants except for baclofen, more strongly inhibits the polysynaptic pathway than the mono-synaptic pathways of the spinal cord as well as more strongly the gamma-system than the alpha-system.
A new method for quantitative grip strength evaluation.