Cyclobenzaprine: a possible mechanism of action for its muscle relaxant effect

1981 ◽  
Vol 59 (1) ◽  
pp. 37-44 ◽  
Author(s):  
John W. Commissiong ◽  
Farouk Karoum ◽  
Rhoderick J. Reiffenstein ◽  
Norton H. Neff
Keyword(s):  
Locus Coeruleus ◽  
Muscle Relaxant ◽  
Muscle Relaxation ◽  
Ventral Horn ◽  
Muscle Rigidity ◽  
Release Of Noradrenaline ◽  
Relaxant Effect ◽  
Decerebrate Rat ◽  
Metabolism Of Noradrenaline ◽  
Thoracic Cord

Intravenously administered cyclobenzaprine (CBZ) (Flexeril), a clinically used, centrally acting muscle relaxant, abolished muscle rigidity in the intercollicular decerebrate rat. In animals in which the locus coeruleus was lesioned bilaterally previously, CBZ failed to attenuate the electromyogram. In the ventral horn of the cord, which receives a dense noradrenergic innervation from the locus coeruleus, CBZ caused an increase in the metabolism of noradrenaline. In the zona intermedia of the thoracic cord, which is not innervated by the locus coeruleus, CBZ caused only minimal effects on noradrenaline metabolism. Cells in the locus coeruleus were activated by CBZ. The results indicate that in the intercollicular decerebrate rat, an intact, coerulospinal, noradrenergic projection is essential for the muscle relaxant effect of CBZ. Muscle relaxation apparently results from an activation of locus coeruleus neurones, leading to an increased release of noradrenaline in the ventral horn of the cord and the subsequent inhibitory action of noradrenaline on α motoneurones.

scholarly journals Muscle Relaxant and Sedative-Hypnotic Activities of Extract ofViola betonicifoliain Animal Models Supported by Its Isolated Compound, 4-Hydroxy Coumarin

2013 ◽  
Vol 2013 ◽  
pp. 1-6 ◽  
Author(s):  
Naveed Muhammad ◽  
Mohammad Saeed ◽  
Haroon Khan ◽  
Achyut Adhikari ◽  
Khalid Mohammed Khan
Keyword(s):  
Muscle Relaxant ◽  
Safety Profile ◽  
Methanolic Extract ◽  
Muscle Relaxation ◽  
Antidepressant Activity ◽  
Relaxant Effect ◽  
Whole Plant ◽  
Hydroxy Coumarin ◽  
Isolated Compound ◽  
Dose Dependent

The crude methanolic extract of the whole plant ofViola betonicifolia(VBME) was investigated for anxiolytic, muscle relaxant, sleep induction, antidepressant, and sedative activities) to ascertain its scientific values. VBME showed a significant (P<0.05) dose dependent anxiolytic action in staircase test. In muscle relaxant paradigms, a dose dependent muscle relaxation was observed. For phenobarbitone sleep induction test, VBME notably (P<0.05) reduced the latency time and increased total sleeping duration. Our tested extract was found free of any antidepressant activity, while the movement was significantly (P<0.05) shortened in locomotor activity. The whole plant ofV. betonicifolialed to the isolation of 4-hydroxyl coumarin (4HC) which showed substantial safety profile in acute toxicity test. When challenged in Traction and Chimney tests, it showed significant (P<0.05) muscle relaxant effect in both muscle relaxant paradigms at 20 and 30 mg/kg during various assessment times. Nevertheless, 4HC was devoid of sedative and hypnotic potentials. In conclusion, VBME had strong muscle relaxant and sedative-hypnotic properties, while its isolated compound, 4HC, possessed a significant muscle relaxant action with substantial safety profile without sedative-hypnotic effects.

A specific benzodiazepine antagonist CGS 8216 reverses the muscle relaxant effect of diazepam but not that of phenobarbitone

1984 ◽  
Vol 98 (3-4) ◽  
pp. 441-444 ◽  
Author(s):  
Waldemar A. Turski ◽  
Michael Schwartz ◽  
Lechoslaw Turski ◽  
Karl-Heinz Sontag
Keyword(s):  
Muscle Relaxant ◽  
Benzodiazepine Antagonist ◽  
Relaxant Effect ◽  
Cgs 8216

THE RATE OF RESIDUAL NEUROMUSCULAR BLOCKADE AFTER LAPAROSCOPIC APPENDECTOMY SURGERY AT NGUYEN TRI PHUONG HOSPITAL

2021 ◽  
Vol 62 (6) ◽  
Author(s):  
Doan Minh Nhut ◽  
Nguyen Van Chinh
Keyword(s):  
Neuromuscular Blockade ◽  
Laparoscopic Appendectomy ◽  
Muscle Relaxant ◽  
Muscle Relaxation ◽  
Cross Sectional Study ◽  
Cross Sectional ◽  
Residual Rate ◽  
Residual Neuromuscular Blockade ◽  
Study Results

Introduction: In Vietnam, using a muscle accelerator to measure the TOF index to monitor residue neuromuscular blockade has not been performed routinely, extubation is mainly based on subjective clinical assessments. Methods: A cross-sectional study on 96 patients undergoing laparoscopic appendectomy at Nguyen Tri Phuong Hospital, from November 2020 to May 2021. Objectives: The study was conducted with 2 objectives including (1) Determine the progression of TOF index at 7 time points: immediately after arriving in the recovery room, after extubation, 15 minutes, 30 minutes, 60 minutes, 90 minutes, 120 minutes after extubation; (2) Determination of residual muscle relaxant rate of patients undergoing laparoscopic appendectomy at Nguyen Tri Phuong Hospital. Results: The average TOF ≥ 0,9 index after laparoscopic appendectomy at the time of resuscitation was 88.11%, extubation was 90.53% and at 120 minutes after extubation. is 99.88%. Residual muscle relaxation after surgery when TOF index < 0.9. At the time of resuscitation, the highest residual rate of muscle relaxant accounted for 58.33%, followed by the time of extubation 39.58%, 15 minutes after extubation was 21.88%. Until 120 after extubation, there is no case that has residue neuromuscular blockade. Conclusion: Through the study results, it is necessary to monitor patients undergoing laparoscopic appendectomy with quantitative devices to more accurately assess the clinical index of muscle relaxation.

A comparison of cyclopiazonic acid and ryanodine effects on cardiac muscle relaxation

1993 ◽  
Vol 265 (4) ◽  
pp. H1364-H1372 ◽  
Author(s):  
N. Pery-Man ◽  
D. Chemla ◽  
C. Coirault ◽  
I. Suard ◽  
B. Riou ◽  
...  
Keyword(s):  
Cardiac Muscle ◽  
Muscle Relaxation ◽  
Cyclopiazonic Acid ◽  
Negative Inotropic Effect ◽  
Inotropic Effect ◽  
Control Group ◽  
Total Force ◽  
Uptake Inhibition ◽  
Relaxant Effect ◽  
Isometric Twitch

We investigated cardiac muscle behavior after inhibition of either sarcoplasmic reticulum (SR) Ca2+ release or SR Ca2+ uptake. Mechanics of 35 rat papillary muscles were studied after either ryanodine 10(-7) M (n = 11) or cyclopiazonic acid (CPA) 10(-5) M (n = 14) and compared with a control group containing the solvent alone (n = 10). We measured the maximum extent of shortening (delta L) of the preloaded twitch (delta Lp), and the normalized total force (TF) of the full isometric twitch (TFi). The peak lengthening velocity (Vl) of the preloaded twitch (Vlp) and the normalized negative peak force derivative of the fully isometric twitch (-DFi) tested the lusitropic state. With the influence of shortening and/or load on relaxation taken into account, analysis of relaxation was performed using 1) Vlp-to-delta Lp and magnitude of -DFi-to-TFi ratios and 2) slopes of the Vl-delta L and magnitude of -DF-TF relationships over the entire continuum of load. Ca(2+)-release inhibition with ryanodine induced a negative inotropic effect and a decrease in Vlp from 2.7 +/- 0.2 to 1.4 +/- 0.2 Lmax/S, where Lmax is the initial length at the peak of the length-active tension curve (P < 0.001). The Vlp-to-delta Lp ratio and the slope of the Vl-delta L relationship were preserved, indicating that ryanodine was devoid of intrinsic relaxant effect under isotonic conditions. Ca(2+)-uptake inhibition with CPA had no inotropic effect but decreased Vlp from 2.9 +/- 0.1 to 2.2 +/- 0.1 Lmax/s (P < 0.001).(ABSTRACT TRUNCATED AT 250 WORDS)

Modulation of vascular tone by neutrophils: dependence on endothelial integrity

1989 ◽  
Vol 257 (4) ◽  
pp. H1315-H1320
Author(s):  
J. L. Mehta ◽  
D. L. Lawson ◽  
W. W. Nichols ◽  
P. Mehta
Keyword(s):  
Smooth Muscle ◽  
Vascular Smooth Muscle ◽  
Muscle Relaxant ◽  
Muscle Tone ◽  
Muscle Relaxation ◽  
Smooth Muscle Relaxation ◽  
Smooth Muscle Tone ◽  
High Concentrations ◽  
Vascular Smooth Muscle Tone ◽  
Smooth Muscle Relaxant

To determine the influence of polymorphonuclear leukocytes (PMNLs) on vascular smooth muscle tone, isolated human PMNLs (10(4)–10(7) cells/ml) were suspended in a tissue bath with precontracted rat aortic rings with or without endothelium. PMNLs in low concentrations (10(4) and 10(5) cells/ml) caused a mild contraction, and in higher concentrations (10(6) and 10(7) cells/ml) caused a modest relaxation of aortic rings with intact endothelium. In contrast, PMNLs caused a potent concentration-dependent relaxation of deendothelialized rings (P less than 0.01 compared with rings with intact endothelium). The PMNL-induced vascular smooth muscle relaxation was abolished by both hemoglobin and methylene blue and potentiated by both superoxide dismutase and captopril. Although suspension of PMNLs caused release of eicosanoids, thromboxane A2 and prostacyclin, from rings with intact endothelium, neither indomethacin nor the TxA2-endoperoxide receptor antagonist SQ 29548 modified the effects of PMNLs on vascular smooth muscle tone. These observations suggest that unstimulated PMNLs generate a smooth muscle relaxant, which has biological characteristics similar to the endothelium-derived relaxing factor. Since the activity of this PMNL-derived smooth muscle relaxant is more pronounced in deendothelialized vascular segments, it appears that endothelium provides a barrier against vasorelaxation by high concentrations of PMNLs.

Muscle relaxant activities of pistagremic acid isolated from Pistacia integerrima

2018 ◽  
Vol 73 (11-12) ◽  
pp. 413-416 ◽  
Author(s):  
Abdur Rauf ◽  
Saud Bawazeer ◽  
Ghias Uddin ◽  
Bina S. Siddiqui ◽  
Haroon Khan ◽  
...  
Keyword(s):  
Muscle Relaxant ◽  
Current Work ◽  
Dependent Manner ◽  
Dominant Effect ◽  
Inclined Plane ◽  
Rotarod Test ◽  
Relaxant Effect ◽  
Muscle Relaxant Activity ◽  
Dose Dependent ◽  
Inclined Plane Test

Abstract The aim of the current work was to explore the muscle relaxant effect of pistagremic acid (PA) isolated from Pistacia integerrima in various animal paradigms. In a rotarod test, PA caused a significant (p<0.05) muscle relaxant potential in a dose-dependent manner. When studied in the inclined plane test, pretreatment with PA (5 and 10 mg/kg) caused promising activity (p<0.05) after treatment for 30, 60 and 90 min. The muscle relaxant potential of PA was strongly complimented by the traction and chimney tests, showing a dominant effect after 60 min of treatment. In conclusion, PA possesses strong muscle relaxant activity in various animal-based models.

scholarly journals Effects of corticotropin-releasing hormone on locus coeruleus neurons in vivo: a microdialysis study using a novel bilateral approach

2001 ◽  
pp. 359-363 ◽  
Author(s):  
S Asbach ◽  
C Schulz ◽  
H Lehnert
Keyword(s):  
Locus Coeruleus ◽  
Fused Silica ◽  
Corticotropin Releasing Hormone ◽  
Release Of Noradrenaline ◽  
Releasing Hormone ◽  
Significant Prolongation ◽  
Bilateral Approach ◽  
Microdialysis Study ◽  
Na Release

OBJECTIVE: Stress-induced release of noradrenaline (NA) from locus coeruleus (LC) neurons is mainly regulated by corticotropin-releasing hormone (CRH). Tyrosine is a precursor of NA and plays an intriguing role in the regulation of NA release. DESIGN: We studied the effects of injecting CRH into the LC using a novel bilateral approach which relies on the mainly ipsilateral projections of LC neurons allowing stimulation of one hemisphere while using the other as control. To analyze the modification of the CRH effect, tyrosine was given intraperitoneally. A combination of CRH and its antagonist d-Phe was administered for validation of the specificity of CRH effects. METHODS: Wistar rats were used in all experiments. Injections were made through fused silica capillaries implanted into both LCs and microdialysis samples were collected bilaterally from the prefrontal cortex (PFM) every 20 min for 1 h before and 3 h after injections. The effects of LC stimulation were investigated by determining 3-methoxy-4-hydroxyphenylglycol (MHPG) in the dialysates. RESULTS: Following CRH injection into one LC and contralateral infusion of artificial cerebrospinal fluid (aCSF), MHPG levels, which are indicative of NA release, increased only in the ipsilateral PFM. These effects were blocked by d-Phe. Simultaneous administration of tyrosine i.p. led to a significant prolongation of MHPG release. CONCLUSIONS: These data provide the first physiological evidence of unilateral LC projections with the bilateral stimulation design proving to be a very valuable tool for the study of LC firing rate, to decrease number of animals and time expenditure. Prolongation of MHPG release after tyrosine supplementation is most likely due to increased NA synthesis.

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