Veratrine
(Synonyms: Cevadine, Cevadin, Cevadene) 目录号 : GC26033Veratridine (Cevadine, Cevadin, Cevadene), a steroidal alkaloid found in plants of the lily family, is a voltage-gated sodium channel activator. Veratridine induces anxiogenic-like behaviors in rats.
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Veratridine (Cevadine, Cevadin, Cevadene), a steroidal alkaloid found in plants of the lily family, is a voltage-gated sodium channel activator. Veratridine induces anxiogenic-like behaviors in rats.
[1] Akiyoshi Saitoh, et al. Behav Brain Res. 2015 Oct 1;292:316-22.
Cas No. | 2/3/8051 | SDF | Download SDF |
别名 | Cevadine, Cevadin, Cevadene | ||
分子式 | C32H49NO9 | 分子量 | 591.73 |
溶解度 | 储存条件 | Store at -20°C | |
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Veratrine-induced reflexes and cough
Respir Med 1991 Jan;85 Suppl A:51-5.PMID:2034836DOI:10.1016/s0954-6111(06)80255-6.
With cats anaesthetized with sodium pentobarbital we studied how veratrine-induced reflexes interact with cough. Cough was elicited by mechanical stimulation of tracheobronchial mucosa and its intensity was evaluated from the changes in oesophageal pressure. Veratrine injected intravenously produced apnoea, bradycardia and long-lasting hypotension. With each dose the intensity of cough was significantly decreased during the apnoea. When the mechanical stimulus was repeated during the breathing following apnoea with remaining hypotension, cough intensity parameters were not changed from control. Veratrine injected intracardially caused bradycardia, hypotension, and decreases in respiratory rate and tidal volume. The intensity of cough elicited just after injection of Veratrine was also significantly decreased. We suggest that veratrine-induced reflexes depress the cough reflex mainly by inhibitory reflexes arising from cardiac receptors. The inhibition of cough is probably mediated indirectly via the inhibition of medullary respiratory neurons.
Effects of Veratrine and paeoniflorin on the isolated rat aorta
J Ethnopharmacol 1999 Sep;66(3):249-55.PMID:10473169DOI:10.1016/s0378-8741(98)00236-0.
The interactions and mechanisms between Veratrine and paeoniflorin on the isolated rat aorta were studied. Veratrine (1x10(-6) to 1x10(-4) g/ml) could induce contraction on the isolated rat aorta in a concentration-related manner. Paeoniflorin had no effect on the isolated rat aorta. Pretreatment with prazosin (1x10(-6) M) and nifedipine (1x10(-6) M) but not yohimbine (1x10(-5) M) could decrease the tension of contraction induced by Veratrine (1x10(-4) g/ml). Sodium nitroprusside (1x10(-4) M) could inhibit the contraction induced by Veratrine (1x10(-4) g/ml) with or without endothelium, whereas methylene blue (5x10(-5) M) could increase the contraction induced by Veratrine (1x10(-4) g/ml). Treatment with Veratrine (1x10(-4) g/ml) could decrease the tension of contraction induced by norepinephrine (1x10(-6) M) or phenylephrine (1x10(-4) M). The inhibition of Veratrine on norepinephrine-induced contraction was potentiated by L-arginine (1x10(-4) M) and reversed by L-NAME (1x10(-5) M). Paeoniflorin (1x10(-4) M) could decrease the tension of contraction induced by Veratrine (1x10(-4) g/ml) and methylene blue (5x10(-5) M). The inhibition of paeoniflorin on Veratrine was more potent on rat isolated aorta with endothelium than without endothelium. Ryanodine (1x10(-5) M) and Ca2+ -free medium could inhibit methylene blue-induced contraction. From the above results, the relaxation of Veratrine on the norepinephrine-induced contraction might be related to the increase of NO and cGMP. The contraction of Veratrine on the isolated rat aorta was via the increase of intracellular calcium which was inhibited by paeoniflorin.
The voltage-gated sodium channel activator Veratrine induces anxiogenic-like behaviors in rats
Behav Brain Res 2015 Oct 1;292:316-22.PMID:26099814DOI:10.1016/j.bbr.2015.06.022.
In this study, we investigated the anxiogenic-like effects of systemically administered Veratrine in rat models of anxiety. In the light/dark test, Veratrine (0.6 mg/kg, s.c.) significantly and dose-dependently decreased the time rats spent in and the number of entries into a light box 30 min after administration, suggesting that Veratrine increases anxiety-like behaviors. These findings were also supported by results from the elevated-plus maze test and the tail-swing behavior test. In addition, Veratrine (0.6 mg/kg, s.c.) significantly increased the plasma concentration of corticosterone, an endogenous biomarker for anxiety, compared to vehicle. On the basis of these results, we conclude that Veratrine induces anxiogenic-like behaviors in rats. The anxiogenic-like behaviors induced by Veratrine (0.6 mg/kg, s.c.) were completely abolished by co-treatment with the typical benzodiazepine anxiolytic diazepam (1 mg/kg, s.c.), when assessed in the elevated-plus maze test. Similar results were obtained with co-treatment with riluzole (10 mg/kg, p.o.), which directly affects the glutamatergic system and has recently been suggested to have anxiolytic-like effects. In conclusion, this study provides evidence that systemically administered Veratrine induces anxiogenic-like behaviors in rats. We propose the Veratrine model as a novel pathological animal model to explore possible candidate drugs for anxiolytics.
Veratrine-stimulated phosphoinositide breakdown as an assay for local anesthetic actions at Na+ channels
Anesth Analg 1995 Sep;81(3):480-5.PMID:7653808DOI:10.1097/00000539-199509000-00009.
The blockade of veratrine-stimulated phosphoinositide breakdown in rat cerebral cortical miniprisms as a model of local anesthetic actions on voltage-dependent sodium channels was assessed. Veratrine stimulated phosphoinositide breakdown with an EC50 value of 5 microM. The stimulation produced by 20 microM Veratrine was blocked completely by (+)-bupivacaine (IC50 7.6 microM [mean of three separate experimental series]), (-)-bupivacaine (IC50 7.3 microM), lidocaine (IC50 34 microM), etidocaine (IC50 3.4 microM), tetracaine (IC50 approximately 2 microM), and prilocaine (IC50 110 microM). Phosphoinositide breakdown responses to ouabain (100-1000 microM) and K+ (50 mM) were only partially blocked by (+)-bupivacaine, and the responses to monensin (100 and 1000 microM) and noradrenaline (30 microM) were not blocked at all by this drug. Nifedipine produced no significant effects on the phosphoinositide response to 10 microM Veratrine. It is concluded that in pulse label experiments using rat cerebral cortical miniprisms, local anesthetics in general, and (+)-bupivacaine in particular, block the phosphoinositide response to Veratrine with a high degree of specificity. This system may be useful as a relatively simple and quantitative assay for drug effects on Na(+)-channels.
Effects of Veratrine and paeoniflorin on isolated mouse vas deferens
Phytomedicine 2002 May;9(4):296-301.PMID:12120810DOI:10.1078/0944-7113-00122.
In this study, we attempted to identify the interactions and mechanisms between Veratrine and paeoniflorin on isolated mouse vas deferens. Paeoniflorin had no effect on isolated mouse vas deferens. Veratrine (1 x 10(-5) approximately 1 x 10(-3) g/ml) could directly induce contraction of isolated rat and mouse vas deferens. The concentration induced by Veratrine (1 x 10(-5) g/ml) was completely inhibited by Ca2+-free solution and verapamil (1 x 10(-5) M), in both the epididymal and the prostatic portions of isolated mouse vas deferens. Naloxone (1 x 10(-5) M) did not alter the contraction induced by Veratrine (1 x 10(-5) g/ml) in either the epididymal or the prostatic portions of isolated mouse vas deferens. Paeoniflorin (4.8 x 10(-5) g/ml) inhibited the contraction induced by Veratrine (1 x 10(-5) g/ml) in both the epididymal and the prostatic portions of isolated mouse vas deferens. Paeoniflorin (4.8 x 10(-5) g/ml) potentiated norepinephrine (1 x 10(-5) M)-induced phasic contraction in the epididymal portion, but decreased contractions in the prostatic portion. Paeoniflorin (4.8 x 10(-5) g/ml) increased KCI (56 mM)-induced phasic contraction in the epididymal portion, but decreased the tonic contraction in either the epididymal or the prostatic portion. Veratrine (1 x 10(-5) g/ml)-induced contractions could be decreased by pretreatment with ryanodine (1 x 10(-5) M) in both the epididymal and the prostatic portions. Pretreatment with the combination of paeoniflorin (4.8 x 10(-5) g/ml) and ryanodine (1 x 10(-5) M) did not potentiate the inhibition of paeoniflorin in the veratrine-induced contraction in both the epididymal and the prostatic portions of isolated mouse vas deferens.