The Effects of Centrally Acting Muscle Relaxants on the Intrathecal Noradrenaline-Induced Facilitation of the Flexor Reflex Mediated by Group II Afferent Fibers in Rats

Alonso

Evidence-Based Complementary and Alternative Medicine

2011

Elenine is the aglycone of elenoside, a cytotoxic arylnaphthalene lignan (NSC 644013-W/1) derived from Justicia hyssopifolia. (Family: Acanthaceae). Elenoside is a β-D-glucoside, with a similar chemical structure to etoposide, exhibiting central depressant activity. In the present study, elenine was given to mice and rats at doses of 10, 20, and 40 mg/kg. Acute toxicity (24 h) and general behaviour in mice was studied as well as its effects on muscular relaxant activity, locomotor activity (Varimex test), and the open-field test and were compared with 10 mg/kg of chlorpromazine. Elenine produced a reduction in the permanence time in muscular relaxant activity (traction test). Spontaneous activity was lower in the Varimex test. The ambulation and rearing were lower compared with the control group, and an increase in boluses was observed in the open-field test. Thus, it can be concluded that elenine has central sedative effects at lower doses than those used with elenoside and has a possible application in conditions of anxiety.

Section: Discussionsupporting

confidence: 88%

Toxicity and Neuropharmacological Effects of Elenine

Alonso

Evidence-Based Complementary and Alternative Medicine

2011

“…Each of these compounds was evaluated a third time in the locomotion assay at a concentration of 100 µM, and subsequently monitored for forebrain electrographic activity. Clorgiline (a monoamine oxidase A inhibitor) and the muscle relaxants zoxazolamine 37 and tolperisone 38 were identified as “false positives” because they reduced swim activity at this concentration but when the same mutant was embedded in agar electrographic seizure events were still observed (see Fig. 6E).…”

Section: Resultsmentioning

confidence: 99%

Drug screening in Scn1a zebrafish mutant identifies clemizole as a potential Dravet syndrome treatment

2013

Dravet syndrome (DS) is a catastrophic pediatric epilepsy with severe intellectual disability, impaired social development and persistent drug-resistant seizures. One of its primary monogenic causes are mutations in Nav1.1 (SCN1A), a voltage-gated sodium channel. Here we characterise zebrafish Nav1.1 (scn1Lab) mutants originally identified in a chemical mutagenesis screen. Mutants exhibit spontaneous abnormal electrographic activity, hyperactivity and convulsive behaviors. Although scn1Lab expression is reduced, microarray analysis is remarkable for the small fraction of differentially expressed genes (~3%) and lack of compensatory expression changes in other scn subunits. Ketogenic diet, diazepam, valproate, potassium bromide and stiripentol attenuate mutant seizure activity; seven other antiepileptic drugs have no effect. A phenotype-based screen of 320 compounds identifies a US Food and Drug Administration-approved compound (clemizole) that inhibits convulsive behaviors and electrographic seizures. This approach represents a new direction in modeling pediatric epilepsy and could be used to identify novel therapeutics for any monogenic epilepsy disorder.

“…showed qualitatively and quantitatively similar effects. It was concluded that tolperisone, as a centrally acting muscle relaxant depresses group II flexor reflex by inhibiting descending noradrenergic tonic facilitation within the spinal cord [20]. …”

Section: Pharmacological Data Of Tolperisone On Whole Animalsmentioning

confidence: 99%

Basic Aspects of the Pharmacodynamics of Tolperisone, A Widely Applicable Centrally Acting Muscle Relaxant

Tekes¹

2014

TOMCJ

Tolperisone (2-methyl-1-(4-methylphenyl)-3-piperidin-1-ylpropan-1-one hydro-chloride) was introduced in the clinical practice more than forty years ago and is still evaluated as a widely applicable compound in pathologically elevated skeletal muscle tone (spasticity) and related pains of different origin. In the present review, basic pharmacodynamic effects measured on whole animals, analyses of its actions on cell and tissue preparations and molecular mechanism of action on sodium and calcium channels are summarized as recently significantly new data were reported.