Differential effects of various Ca2+ antagonists

Farré, A.J.; Colombo, M.; Fort, Maria; Gutiérrez, Benjamín

doi:10.1016/0306-3623(91)90331-y

Cited by 136 publications

(120 citation statements)

References 8 publications

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“…To assess whether the sapsmolytic activity of the plant extract was through calcium channel blockade, the tissue preparation were depolarized by exposing to high concentration of KCl, i.e., K + (80 mM), resulting in appearance of sustained contraction as previously described (Farre et al, 1991).…”

Section: Determination Of Ca +2 Channel Blocking Activitymentioning

confidence: 99%

Pharmacological basis for the folkloric uses of Buxus wallichiana in gastrointestinal, respiratory and vascular disorders

Hussain

Raza

Janbaz

2015

Bangladesh J Pharmacol

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In vitro study was carried out to explore the pharmacological basis of crude extract of Buxus wallichiana for its folkloric uses in gastrointestinal, respiratory and vascular disorders. In jejunum preparations, crude extract (0.03 ± 1.0 mg/mL) caused a transient spasmogenic effect followed by the spasmolytic effect at higher doses (3.0–10 mg/mL). In atropinized jejunum preparation, crude extract inhibited the spontaneous and K+ (80 mM)-induced contraction, suggesting that spasmolytic effect is mediated through the Ca+2-channel blockade. The Ca+2-channel blockade effect was confirmed when pretreatment of tissue with extract produced a dose-dependent shift in Ca+2 concentration-response curves to the right, similarly as verapamil. Furthermore, crude extract exhibited non-specific relaxant effect on carbachol- (1 µM) and K+ (80 mM)-induced tracheal contractions, suggesting the coexistence of anticholi-nergic and Ca+2-antagonistic properties. Moreover, it relaxed the K+ (80 mM)- and phenylephrine (1 µM)-induced contraction in rabbit aorta, suggesting the Ca+2-channel blockade. These findings may validate the folkloric uses of B. wallichiana in constipation, bronchitis, asthma and hypertension.

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Section: Determination Of Ca +2 Channel Blocking Activitymentioning

confidence: 99%

Pharmacological basis for the folkloric uses of Buxus wallichiana in gastrointestinal, respiratory and vascular disorders

Hussain

Raza

Janbaz

2015

Bangladesh J Pharmacol

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“…Each tissue was allowed to equilibrate for at least 30 min before the addition of any drug. Calcium channel blocking activity of compound 4 was determined as described by Farre et al [26].…”

Section: Antispasmodic Assaysmentioning

confidence: 99%

New natural cholinesterase inhibiting and calcium channel blocking quinoline alkaloids

Atta-ur-Rahman

Khalid

Sultana

et al. 2006

Journal of Enzyme Inhibition and Medicinal Chemistry

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During this study, one new coumarin; 7-O-b-D-glucopyranoside-2H-1-benzopyran-2-one (1) and three quinoline alkaloids; 3-hydroxy, 2, 2, 6-trimethyl -3, 4, 5, 6-tetrahydro-2H-pyrano[3,2-c] quinoline 5-one (2), ribalinine (3) and methyl isoplatydesmine (4) were isolated from the aerial parts of Skimmia laureola and their structures established by spectroscopic studies. Compounds 2-4 were found to be linear mixed type inhibitors of acetylcholinesterase (K i ¼ 110.0, 30.0 and 30.0 mM, respectively). Compounds 2 and 3 were also found to be linear mixed type inhibitors of butyrylcholinesterase, while compound 4 was a noncompetitive inhibitor of the enzyme (K i ¼ 90.0, 70.0 and 19.0 mM, respectively). The inhibition of acetyl-and butyryl-cholinesterase enzymes persists as the most promising therapeutic strategy for activating the impaired cholinergic functions in Alzheimer's disease and related dementias.Compound 4 also showed dose-dependent spasmolytic activity in the isolated rabbit jejunum intestinal preparation by relaxing the spontaneous (EC 50 ¼ 0.1 mg/mL) and K þ -induced contractions (EC 50 ¼ 0.4 mg/mL), suggesting that the spasmolytic effect of compound 4 is mediated through the blockade of voltage-dependent Ca 2 þ channels.

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“…To assess the mechanism of spasmolytic activity of the test substances, it was mediated through calcium channel blockade, a high concentration of K + (80 mM), as KCl, was added to depolarize the tissue preparations (Farre et al, 1991). The added K + (80 mM) produced a sustained contraction.…”

Section: Effect On the High K + -Induced Contractionmentioning

confidence: 99%

Ethnopharmacological evaluation of Cenchrus ciliaris for multiple gastrointestinal disorders

Aleem

Janbaz

2017

Bangladesh J Pharmacol

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This study was conducted to rationalize the traditional uses of Cenchrus ciliaris in gastrointestinal disorders using in vivo and ex vivo assays. The antidiarrheal effect was evaluated in rats by the castor oil-induced diarrheal model. C. ciliaris (100, 300 and 500 mg/kg) reduced the castor oil-induced diarrhea significantly. Another study carried out in mice to determine the intestinal transit rate showed that C. ciliaris (100 and 200 mg/kg) inhibited the transit rate significantly. Ex vivo assay demonstrated that C. ciliaris (0.01–1 mg/mL) relaxed the spontaneous and K+ (80 mM)-induced contractions, like verapamil. The crude extract (75, 100 and 150 mg/kg) also exhibited significant anti-emetic activity in chicks. These results indicate the presence of antispasmodic, antidiarrheal and antiemetic activities in C. ciliaris, thus providing the scientific basis for its traditional uses.Video Clip of Methodology: 56 sec <a href="https://www.youtube.com/v/FwQ01gHJaGk">Full Screen</a> <a href="https://www.youtube.com/watch?v=FwQ01gHJaGk">If Failed</a>

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Differential effects of various Ca2+ antagonists

Cited by 136 publications

References 8 publications

Pharmacological basis for the folkloric uses of <i>Buxus wallichiana</i> in gastrointestinal, respiratory and vascular disorders

Pharmacological basis for the folkloric uses of <i>Buxus wallichiana</i> in gastrointestinal, respiratory and vascular disorders

New natural cholinesterase inhibiting and calcium channel blocking quinoline alkaloids

Ethnopharmacological evaluation of Cenchrus ciliaris for multiple gastrointestinal disorders

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