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At least 253 records · Page 14Linked to original sources
PubMed1995

Spasmolytic and calmodulin inhibitory effect of non-steroidal anti-inflammatory drugs in vitro.

The effect of several anti-inflammatory drugs (NSAIDs), the calmodulin inhibitor W-7 and cortisol on vanadate-induced tonic contraction and on calmodulin dependent cAMP-phosphodiesterase activity have been assayed. Indomethacin, diclofenac, phenylbutazone, mefenamic acid, naproxen, tolmetin, piroxicam, aspirin and W-7, but not metimazol, produce dose-dependent relaxation of vanadate-induced tonic contraction on isolated rat uterus. Cortisol relaxes the vanadate contraction up to 45%. None of the drugs assayed inhibit the basal activity of phosphodiesterase with concentrations lower than 1 mM. However, indomethacin, diclofenac, phenylbutazone, mefenamic acid, naproxen, piroxicam, aspirin and W-7 inhibit, in a concentration-dependent way, the calmodulin-stimulated activity of phosphodiesterase. The maximum inhibition achieved with tolmetin (1 mM) and cortisol (1 mM) was 38% and 24%, respectively. Metamizol has no effect on basal or/and stimulated phosphodiesterase. This, as far as we know, is the first description of relationship between NSAIDs and calmodulin-dependent processes and our results suggest that the inhibition of calmodulin with NSAIDs may be directly related to their pKa and liposolubility.

3',5'-Cyclic-AMP Phosphodiesterases↗
PubMed1980

The spasmolytic properties of 5-chloro-4-(2-imidazolin-2-yl-amino)-2, 1,3-benzothiadiazole hydrochloride (DS 103-282): a pilot study.

The overall efficacy and tolerance of a new skeletal muscle relaxant DS 103-282 was evaluated by treating 10 patients with chronic spinal spasticity. Other agents such as baclofen, dantrolene sodium or diazepam had been only minimally beneficial in these patients. Treatment was started with DS 103-282 at a mean dosage of 7.4 mg. per day which was adjusted according to response up to 14.5 mg. per day at the end of the 8-week trial period. Objective rating assessments showed improvement in spasticity, medullary automatism and clonus. No changes were recorded in the reflex pattern nor improvement in disability scores. Only a few mild side-effects were reported, there was a noticeable absence of sedation, but reduction in systolic and diastolic blood pressure was noted in most patients. DS 103-282 appears to have demonstrable myotonolytic action and in view of its good tolerance it deserves further investigation.

Adult↗
PubMed1984

Time course of the spasmolytic effect of cadmium and cadmium uptake in guinea-pig taenia coli.

The relationship between tension inhibitory action of cadmium and cadmium uptake was investigated in the smooth muscle of taenia coli. Following a treatment with 0.5 mM Cd2+ for short periods (1, 5 min), the tension to high-K+ returned to a greater extent after washing with disodium edetate (EDTA) or cysteine, compared to normal medium. However, the restored tension to the high-K+ decreased with increasing duration of Cd2+ treatment. With a longer duration of 0.5 mM Cd2+ treatment, the cadmium uptake increased and the size of cadmium fraction bound to cells firmly increased. It is suggested that Cd2+ binds initially to the surface membrane of taenia coli and that Cd2+ subsequently migrates to a compartment that EDTA cannot reach.

Animals↗
PubMed1995

Involvement of sodium/calcium exchange in the diclofenac-induced spasmolytic effect on rat uterus.

1. The effect of diclofenac (10-100 microM) on rat uterus contraction and its modification by ouabain (0.1 mM), amiloride (0.1 and 1 mM), ouabain (0.1 mM) plus amiloride (1 mM) and the replacement of sodium by choline have been assayed. 2. Diclofenac produces dose-dependent relaxation of vanadate (0.3 mM)-induced contraction (EC50, 17.3 +/- 1.8 microM). This effect is significantly reduced in choline medium (EC50, 49.1 +/- 4.5 microM) and by ouabain in sodium-medium (EC50, 52 +/- 7 microM). 3. Amiloride displaces, in a dose-dependent way, the diclofenac-induced relaxant effect. However, ouabain plus amiloride did not produce a sinergic effect. 4. Our results suggest that diclofenac produces relaxation of vanadate-induced contraction by activation of Na+/Ca(2+)-exchange.

Amiloride↗
PubMed1996

Mechanisms involved in the spasmolytic effect of extracts from Sabal serrulata fruit on smooth muscle.

1. The effects of two extracts from Sabal serrulata fruits [total lipidic (L) and saponifiable (S)] on smooth muscle contractions have been assayed. 2. Both extracts (0.1-1 mg/ml) relaxed the tonic contraction induced by norepinefrine (30 nM) on rat aorta [EC50, 0.53 +/- 0.05 mg/ml (L) and 0.5 +/- 0.04 mg/ml (S)] and by KCl (60 mM) on rat uterus. The Sabal extracts (0.3-1 mg/ml) also antagonized the dose-response curve of contractions induced by acetylcholine (0.1-100 microM) on urinary bladder. 3. dL-Propranolol (1 microM) but not the inactive (R)-(+)-propranolol(1 microM) potentiated the Sabal extracts relaxant effect by lowering the EC50 (0.35 +/- 0.2 vs 0.20 +/- 0.01 mg/ml for L and 0.43 +/- 0.02 vs 0.19 +/- 0.02 mg/ml, P < 0.01, for S extract). 4. Cycloheximide (10 micrograms/ml) antagonized the effect of extracts from Sabal. However, actinomycin D (5 micrograms/ml) significantly (P < or = 0.01) antagonized the effect of the total lipidic extract without modifying that of the saponifiable extract. 5. The relaxant effect of both extracts was not modified by the tyrosine kinase inhibitor genistein (10 microM) or the ornithine decarboxylase inhibitor alpha-difluoromethyl-ornithine (10 mM).

Adrenergic beta-Antagonists↗
PubMed1990

Intestinal smooth muscle spasmolytic actions of the aqueous extract of the roots of Taverniera abyssinica.

A room temperature aqueous extract of the roots of Taverniera abyssinica antagonized the contractile responses of the guinea-pig ileum to acetylcholine and histamine. The extract also relaxed the smooth muscle of the rabbit duodenum, abolished the pendular contractions and antagonized the effects of acetylcholine and histamine on this tissue. The results confirm that there may be a sound pharmacological basis for the ethnomedical use of the roots of this plant to treat stomach ache.

Acetylcholine↗
PubMed2004

Spasmolytic stilbenoids from Maxillaria densa.

2,5-dihydroxy-3,4-dimethoxyphenanthrene (1), fimbriol-A (2), nudol (3), gymnopusin (4) and erianthridin (5) isolated from Maxillaria densa provoked a concentration-dependent inhibition of the spontaneous contractions of the rat ileum with potencies comparable to papaverine. In order to establish the mode of action of stilbenoids 1-5, their effect on the contractions induced by different spasmogens (histamine, barium chloride and L-NAME) was investigated. In general, the results suggested that the relaxant activity of the products does not involve a direct nitrergic or antihistaminergic mode of action or an interference with calcium influx into the smooth muscle cells.

Animals↗
PubMed2006

Intestinal spasmolytic effects of STW 5 (Iberogast) and its components.

Functional gastro-intestinal diseases as the irritable bowel syndrome are very common in the population and are characterized by a broad spectrum of symptoms which mostly are related to spastic or paralytic intestinal function without defined histopathological changes of the tissue. Due to the multifactorial pathogenesis a multifactorial therapy with multi-target action seems to be reasonable. STW 5 (Iberogast), its constituent herbal extracts and some isolated compounds were used in an in vitro model provided by intestinal samples from guinea pig in order to test their activity on histamine-induced contractions and spontaneous motility, respectively. For comparison the known spasmolyticum papaverine was used. The results show that the lytic effect of the phytotherapeuticum on histamine-induced contraction represents additively the actions of the different components and corresponds to approx. 10 microM of papaverine. Spontaneous peristaltic motion was differently modulated by the various constituent extracts. The experiments with silibinin, glycyrrhicine, chelidonine, and protopine showed that the effects of the extracts were not comparable to those of the respective chemical constituents.

Animals↗
PubMed2000

Mechanism of mifepristone-induced spasmolytic effect on isolated rat uterus.

Mifepristone, a synthetic 19-norsteroid, relaxed the KCl-induced tonic contraction in isolated rat uterus in a concentration-dependent way and CaCl2 (0.1 to 10 mM) counteracted it. This effect was similar to other steroids although the mechanisms involved are unclear. Before adding the contracturant, tissue was incubated with actinomycin D (10 microM), cycloheximide (300 microM), TPCK (3 and 10 microM), Rp-cAMPS (30 microM), DDA (100 microM) and H-7 (1 microM). None of these modified the relaxing effect of mifepristone. Incubation with drugs that interfere with cGMP such as a nucleotide analogue DDG (100 microM), a soluble guanylyl cyclase inhibitor ODQ (1 microM) and an inhibitor of protein kinase G 8pCPTcGMPS (1 microM) significantly modified the effect of mifepristone, increasing its IC50.

Animals↗
PubMed1997

Spasmolytic effect of water extract of Stemonae radix on the guinea-pig tracheal smooth muscle in vitro.

The present study examined the relaxing effect of a water extract of Baibu (Stemonae radix, the root tuber of Semona sessilifolia (Miq.) Franch. et Sav.) on carbachol-, histamine- and KCl-induced contractions of the guinea-pig isolated tracheal preparations. The results showed that Baibu (1-50 mg/ml) concentration-dependently relaxed the tracheal preparations contracted by these spasmogens with an IC50 value (mg/ml) of 2.0 +/- 0.1 for carbachol, 41.2 +/- 0.8 for histamine and 18.6 +/- 0.9 for KCl. The effect of Baibu was not affected by the pretreatment with a beta-adrenoceptor antagonist propranolol (10(-6) M), indicating that Baibu's effect was not due to an activation on beta-adrenoceptors. Baibu shifted the concentration-response curve of carbachol to the right in a parallel manner without changing the maximal response, having a pA2 value of 0.16 +/- 0.07 mg/ml (equivalent to a KB = 0.70 +/- 0.11 mg/ml). This indicates a competitive antagonism at the muscarinic receptors. Receptor binding assay indicated that Baibu interacted with the muscarinic receptors (Ki = 0.51 +/- 0.12 mg/ml) and the dihydropyridine (DHP) binding site of L-type Ca2+ channels (Ki = 8.0 +/- 1.9 mg/ml), but not with the histamine H1 receptors. Therefore, the present study demonstrates that Baibu contains the principle(s) acting on the muscarinic receptors and DHP binding sites, which contribute its relaxation effect on the airway smooth muscles.

Animals↗
PubMed2003

Determination of binary mixtures of analgesic and spasmolytic drugs in pure and dosage forms by derivative spectrophotometry.

Binary mixtures of dipyrone and pitophenone hydrochloride are assayed by zero-crossing second- and third-derivative spectrophotometry and by ratio-spectra first- and second-derivative spectrophotometry. In the first method, calibration plots are linear at 266.5 and 302.5 nm (dipyrone, second derivative), and 257 and 286 nm (pitophenone second derivative) and 242 and 278.3 nm (dipyrone third derivative), and 228.5 and 300 nm (pitophenone, third-derivative). By the second method, lines of regression are linear at 235 and 262 nm (dipyrone, first derivative), and 229.5 and 288.5 nm (pitophenone, first-derivative), and 249.7 and 268 nm (dipyrone, second derivative), and 280.5 and 300 nm (pitophenone, second-derivative). In all methods calibration curves follow the Beer's law up to 40 microg/ml of each drug. LOD and LOQ values were calculated. The developed derivative spectrophotometric methods were applied to laboratory mixtures and to vials for these drugs. The procedures are simple, rapid, and did not require any preliminary separation or treatment of the samples.

Analgesics↗