The relaxant effect of curcumin on porcine coronary arterial ring segments

2007 ◽  
Vol 47 (1) ◽  
pp. 25-30 ◽  
Author(s):  
Pei-Han Xu ◽  
Yuan Long ◽  
Fang Dai ◽  
Zhong-Li Liu
Keyword(s):  
Relaxant Effect ◽  
Arterial Ring

scholarly journals Lack of synergistic interaction between quercetin and catechin in systemic and pulmonary vascular smooth muscle

2010 ◽  
Vol 105 (9) ◽  
pp. 1287-1293 ◽  
Author(s):  
Carmen Menendez ◽  
Rosario Jimenez ◽  
Laura Moreno ◽  
Pilar Galindo ◽  
Angel Cogolludo ◽  
...  
Keyword(s):  
Endothelial Dysfunction ◽  
Vascular Function ◽  
Pulmonary Arteries ◽  
Rat Aorta ◽  
Relaxant Effect ◽  
Isobolographic Analysis ◽  
Scavenging Effect ◽  
Synergistic Interactions ◽  
Pure Compounds ◽  
Intermediate Effect

Due to their ubiquitous distribution, flavonoids from different classes are commonly present together in foods. However, little is known about the interactions between them. The flavonol quercetin and the flavan-3-ol (+)-catechin are among the most abundant flavonoids in the diet. In the present study, we have analysed the interactions between these two flavonoids on vascular function using two pure compounds and mixtures of these flavonoids in 1:0·1, 1:1 or 1:10 proportions. Quercetin induced a more potent concentration-dependent relaxant effect than catechin in the isolated rat aorta, and the isobolographic analysis of the mixtures showed no synergistic or antagonistic effects between them, i.e. their effects were additive. Quercetin was more potent in mesenteric than in pulmonary arteries. Catechin had weak effects in these vessels and did not modify the effects of quercetin. Endothelial dysfunction induced by increased oxidative stress by the superoxide dismutase inhibitor diethyldithiocarbamate was prevented by quercetin, whereas catechin showed a weak effect and the 1:1 mixture an intermediate effect compared with the pure compounds. Quercetin but not catechin showed a pro-oxidant and NO-scavenging effect, which was not prevented by catechin. In conclusion, catechin was less potent than quercetin as a vasodilator, pro-oxidant or to prevent endothelial dysfunction, and there were no synergistic interactions between quercetin and catechin.

scholarly journals Pharmacological characterization of the relaxant effect induced by adrenomedullin in rat cavernosal smooth muscle

2014 ◽  
Vol 47 (10) ◽  
pp. 876-885
Author(s):  
L.N. Leite ◽  
N.A. Gonzaga ◽  
D.P.C. Tirapelli ◽  
L.F. Tirapelli ◽  
C.R. Tirapelli
Keyword(s):  
Smooth Muscle ◽  
Pharmacological Characterization ◽  
Relaxant Effect

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 relaxant effect of nifedipine in human uterine smooth muscle and the BKCa channel

2008 ◽  
Vol 198 (2) ◽  
pp. 237.e1-237.e8 ◽  
Author(s):  
Audrey T. Moynihan ◽  
Terry J. Smith ◽  
John J. Morrison
Keyword(s):  
Smooth Muscle ◽  
Bkca Channel ◽  
Relaxant Effect ◽  
Uterine Smooth Muscle

scholarly journals The effect of lemborexant for insomnia disorder

2021 ◽  
Vol 9 ◽  
pp. 205031212110390
Author(s):  
Hidenobu Suzuki ◽  
Hiroyuki Hibino
Keyword(s):  
Clinical Practice ◽  
Average Dose ◽  
Relaxant Effect ◽  
Athens Insomnia Scale ◽  
Subjective Evaluations ◽  
Duration Of Illness ◽  
Insomnia Disorder ◽  
Efficacy Outcome ◽  
The Mean ◽  
Objective Indicators

Background: Lemborexant has a low dependence potential, less muscle relaxant effect, and less effect on cognitive function. However, there have been no naturalistic reports in Japan clarifying the effect of lemborexant on insomnia disorder. We retrospectively examined the effectiveness of treatment with lemborexant. Methods: Insomnia was assessed using the Athens Insomnia Scale (AIS). Efficacy outcome assessment was the Clinical Global Impressions–Improvement scale (CGI-I). Results: We analyzed 150 patients (male/female = 57/93) in total. The mean subject age and mean duration of illness were 47.8 ± 19.9 years and 4.2 ± 7.2 years, respectively. The average dose of lemborexant was 5.9 ± 2.0 mg. The mean AIS total score was a significant improved (6.6 ± 3.7–3.9 ± 3.3) ( p < 0.01). The mean CGI-I score was 3.2 ± 0.8. The 24-week continuation rates for lemborexant were 86.7%. Conclusion: Similar to the results obtained in previous studies, the CGI-I score, which is one of the objective indicators evaluated by the therapist, and the AIS, which is one of the subjective evaluations of patients, improved as well. The results of this study suggest that lemborexant may be safe and effective in patients with insomnia in real-world clinical practice.

scholarly journals Relaxant effect of quercetin on rabbit isolated bladder smooth muscles contractions

2020 ◽  
Vol 10 (1) ◽  
pp. 61-67
Author(s):  
Hassan Sadraei ◽  
Sabihe Tabesh
Keyword(s):  
Smooth Muscles ◽  
Electrical Field Stimulation ◽  
Negative Control ◽  
Flavonoid Compound ◽  
Drug Candidate ◽  
Control Group ◽  
Organ Bath ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Relaxant Effect

Introduction: Quercetin is a flavonoid compound found in many medicinal plants. Antispasmodic effect of quercetin has been reported in ileum and uterus smooth muscles but not in bladder. Therefore, the objective of this research was to investigate relaxant effect of quercetin in rabbit isolated bladder. Methods: Male rabbit was asphyxiated with carbon dioxide and then sacrificed. The whole bladder was dissected out and placed in oxygenated Tyrode’s solution. Isolated bladder was cut into longitudinal strips and placed in an organ bath for contraction studies. Contractions were induced with KCl (20mM), acetylcholine (5μM) and electrical field stimulation (EFS). Full inhibitory concentration–response curve was constructed for quercetin following addition of above spasmogens. Quercetin was added into the organ bath with 2 fold increments in concentration until maximum response was achieved. Nifedipine was used as positive control group and equivalent volume of quercetin vehicle (water + DMSO) was used as negative control group.Results: Quercetin (4 μg/mL to 640 μg/mL) in a concentration dependent manner inhibited isolated bladder strips contracted by KCl (IC50=159±25 μg/mL), acetylcholine (IC50=43±9.1 μg/mL) and EFS (IC50=38±9.3 μg/mL). In the highest used concentration, quercetin completely removed contractile responses to KCl, acetylcholine and electrical filed stimulation (EFS). Nifedipine totally inhibited KCl response (IC50=115±36 ng/mL) but only partially inhibited acetylcholine and EFS responses. Conclusion: These results confirm the relaxant effect of quercetin on rabbit bladder and if similar effects are seen in human studies, then quercetin would be a suitable drug candidate to be investigated for bladder incontinence.

scholarly journals Characteristic of the vasorlaxant action of the talatisamine alkaloid and its derivatives

2021 ◽  
Vol 4 (2) ◽  
pp. 01-05
Author(s):  
Mirzayeva Yu.T.
Keyword(s):  
Sarcoplasmic Reticulum ◽  
Channel Blocker ◽  
Aortic Ring ◽  
Diterpenoid Alkaloids ◽  
Relaxant Effect ◽  
Ring Contraction ◽  
Voltage Dependent ◽  
Ca2 Channels ◽  
Isolated Rat

The aim of our research is to study the effect relaxant action of diterpenoid alkaloids talatisamine, 14-O-benzoylthalatisamine and 14-O-acetylthalatisamine was studied using isolated rat aortic rings. Alkaloids significantly and dose-dependently inhibited contraction of the aortic rings caused by high KCl content. At the same time, under these conditions, alkaloids significantly reduced Ca2+-induced contraction of the aortic rings. The relaxing effects of alkaloids are significantly suppressed by verapamil, a potent potentiometer-dependent Ca2+ channel blocker. The alkaloids also significantly reduced norepinephrine-induced aortic ring contraction in normal as well as Ca2+ free Krebs solutions. The data obtained indicate that talatisamine, 14-benzoylthalatisamine and 14-O-acetylthalatisamine exhibit a pronounced relaxant effect in almost the same way in the case of contraction induced by a high content of KCl and norepinephrine. The mechanism of the relaxant action of alkaloids is probably complex and may include suppression of Ca2+influx through voltage-dependent and receptor-driven Ca2+ channels, as well as inhibition of Ca2+transport in the sarcoplasmic reticulum.

Interplay of VIP and nitric oxide in regulation of the descending relaxation phase of peristalsis

1993 ◽  
Vol 264 (2) ◽  
pp. G334-G340 ◽  
Author(s):  
J. R. Grider
Keyword(s):  
Nitric Oxide ◽  
Smooth Muscle ◽  
Protein Kinase ◽  
Protein Kinase G ◽  
Rat Colon ◽  
No Production ◽  
Field Stimulation ◽  
Relaxant Effect ◽  
Relaxation Phase ◽  
Kinase A

Involvement of vasoactive intestinal peptide (VIP) and nitric oxide (NO) in neurally induced relaxation was examined in smooth muscle from rat colon. Relaxation induced by field stimulation or radial stretch (i.e., descending relaxation phase of the peristaltic reflex) was accompanied by VIP release and NO production. NG-nitro-L-arginine (L-NNA) abolished NO production in both preparations but only partly inhibited VIP release (45 +/- 8% at 8 Hz and 59 +/- 10% at 10 g stretch) and relaxation (62 +/- 5% and 35 +/- 6%); the effect of L-NNA was reversed by L-arginine but not D-arginine. The pattern implied that NO production normally acts to enhance VIP release. In addition, VIP induced relaxation and stimulated NO production in muscle strips and isolated colonic muscle cells: L-NNA abolished NO production but only partly inhibited relaxation (58 +/- 6%); oxyhemoglobin had no effect. The effect of L-NNA on relaxation was reversed by L-arginine but not by D-arginine. The protein kinase A inhibitor (R)-p-adenosine 3',5'-cyclic phosphorothioate [(R)-p-cAMPS] and the protein kinase G inhibitor KT5823 inhibited VIP-induced relaxation by 76 +/- 5 and 35 +/- 4%, respectively; a combination of the two inhibitors abolished relaxation. (R)-p-cAMPS blocked the direct relaxant effect of VIP, whereas KT5823 blocked the indirect effect of VIP mediated by NO.(ABSTRACT TRUNCATED AT 250 WORDS)

Responses of the isolated rectum of the rainbow lizard (Agama agama) to sympathomimetics

1989 ◽  
Vol 67 (1) ◽  
pp. 68-71
Author(s):  
A. L. Inyang ◽  
D. T. Okpako
Keyword(s):  
Inhibitory Response ◽  
Relaxant Effect ◽  
Dose Dependent ◽  
Noradrenaline And Adrenaline

The relaxant effects of isoprenaline, noradrenaline, and adrenaline on the isolated rectum of the rainbow lizard (Agama agama) were studied. Responses were measured as a reduction of carbachol-induced contractions for each sympathomimetic agent. Isoprenaline, adrenaline, noradrenaline produced a dose-dependent relaxation of this preparation and the order of potency was as given. The pD2 value of 8.15 ± 1.88 obtained for isoprenaline was significantly different (p < 0.05) from those for adrenaline (5.80 ± 0.90) and noradrenaline (5.25 ± 1.18). H35/25, propranolol, and practolol competitively antagonized the relaxant effects of isoprenaline on the isolated lizard rectum. The pA2 values for these β-adrenoceptor antagonists did not differ significantly (at p < 0.05). α-Adrenoceptor antagonists, phentolamine and phenoxybenzamine, failed to alter the relaxant responses of these sympathometics to any appreciable extent. These results are interpreted to suggest that the relaxant effect produced by these sympathomimetics are mediated predominantly by β-adrenoceptors that are not significantly differentiated into subtypes, α-Adrenoceptors in this preparation contribute minimally to the observed inhibitory response following sympathomimetic stimulation.Key words: sympathomimetics, lizard rectum, inhibitory response, β-receptors, α-receptors.

Sign in / Sign up

Export Citation Format

Share Document