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At least 91 records · Page 5Linked to original sources
PubMed1988

Calcium antagonistic and spasmolytic activities of a new 1,5-benzothiazepine derivative in isolated canine and monkey arteries.

Effects of TA-3090 ((+) (2S,3S)-3-acetoxy-8-chloro-5-(2-(dimethylamino)ethyl)-2, 3-dihydro-2-(4-methoxyphenyl)-1,5-benzothiazepin-4-(5H)-one maleate)and diltiazem on contractions induced by different spasmogens were investigated in isolated canine and monkey arteries. Ca2+-antagonistic action in canine arteries, assessed by suppression of Ca2+-induced contraction in Ca2+-free, K+-depolarizing solution, was as follows; basilar (pA2 = 8.34) greater than coronary (pA2 = 7.95) greater than renal (pA2 = 7.46) = mesenteric artery (pA2 = 7.36). The potency of TA-3090 was 10 times greater in basilar artery and 2 to 3 times greater in the other arteries than that of diltiazem. The effect of TA-3090 on the arterial segment was more persistent than that of diltiazem. Relative vasorelaxing potency of TA-3090 to diltiazem in K+-induced contractions was greatest in the basilar artery among the tested arteries of both monkeys and dogs. Spasmolytic activities of TA-3090 on 5-HT-, PGF2 alpha-, U-46619 (thromboxane A2/prostaglandin H2 agonist) and oxyhemoglobin-induced contractions in canine basilar arteries were more potent than those of diltiazem, especially on 5-HT-induced contraction. In addition, TA-3090 suppressed 3,4-diaminopyridine-induced rhythmic contraction in the canine coronary artery. These results indicate that TA-3090 has potent Ca2+-antagonistic and spasmolytic activities, and these actions are most selective for basilar artery.

15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5↗
PubMed1987

N-butyl hyoscine exerts local spasmolytic effect in the small and large bowel of the conscious dog.

The spasmolytic activity of N-Butyl Hyoscine (NBH) (1) has been investigated in conscious dogs provided with ileal or colonic Thiry fistulas in which motility was stimulated by intraluminal distension. In ileal motility experiments, phasic motility index (PMI), intestinal tonus, contraction frequency and heart rate were monitored. Intravenous administration of NBH (10 to 100 micrograms/kg) depressed PMI (ED50 35.1 micrograms/kg) and the other motility parameters. Heart rate increases were observed at 100 micrograms/kg. Application of NBH directly into the fistula (300 to 3000 micrograms/kg) caused a long-lasting, potent inhibition (31-72%) of PMI; tonus and contraction frequency were only slightly affected, while heart rate was not altered. When NBH was administered into an ileal fistula adjacent to the one from which motility was recorded, changes of PMI and other parameters were observed only after a massive dose of the drug (10000 micrograms/kg). In colonic fistula experiments, intraluminal NBH administration (300 to 3000 micrograms/kg) depressed colonic motility (39-59%), without affecting heart rate. It is concluded that NBH present in the intestine, although poorly absorbed, exerts local spasmolytic action.

Animals↗
PubMed1977

[Studies on the mechanism of action of vascular spasmolytics. 3. Effect of nitroprusside sodium, nitroglycerin, prenylamine and verapamil on the fluoride-induced contracture of the isolated coronary artery].

On isolated coronary arteries of cattle, nitroprusside-sodium, nitroglycerol, prenylamine, and verapamil were studied for their spasmolytic effects on a contracture induced by fluoride ions. With this contracture model, which is independent of extracellular calcium, nitroprosside-sodium and nitroglycerol showed strong spasmolytic action. Verapamil proved ineffective, and the effectiveness of prenylamine was strongly reduced. The results lend support to earlier findings suggesting that nitroglycerol and nitroprusside-sodium are endowed with a relaxation mechanism different from that of verapamil and analogously acting compounds.

Animals↗
PubMedDate not supplied

[Spasmolytic properties of pyrrolizidine alkaloids].

Acute toxicity, spasmolytic and hypotensive properties of the alkaloids senecionine, d-otocenine and floridanin isolated from Senecio Erraticum L. were studied. D-otocenine and floridanin elicited low toxicity, while senecionine and d-otosenine showed spasmolytic and floridanin predominantly hypotensive properties.

Animals↗
PubMedDate not supplied

Antagonism of calcium-induced contractions by some non-specific spasmolytics in depolarized smooth muscles.

The effects of papaverine MgCl2, cocaine, DNP, KCN and khellin on responses of some rabbit and rat tissues to CaCl2 were studied in vitro in a depolarizing medium. Guinea pig taenia coli preparation was used for comparison. In rabbit tracheal chain and vas deferens and guinea pig taenia coli preparations all spasmolytics shifted the concentration-response curves of CaCl2 to the right without affecting the maxima or slopes. In rat tracheal chain and vas deferens preparations all spasmolytics shifted the concentration-response curves of CaCl2 to the right. Furthermore all agents (except cocaine in tracheal chain preparations) depressed the maximum responses. The slopes were unaffected in either preparations. The initial competition and subsequent noncompetition observed in certain tissues is discussed in the light of the reported poor capacity of some tissues to retain Ca++ and the absence of releasable firmly bound Ca++ (11).

Animals↗
PubMed1977

[On the spasmolytic action of 3-butoxy-1-phenoxy-propanol-(2) (febuprol) on the biliary tract (author's transl)].

The spasmolytic activity of 3-butoxy-1-phenoxy-propanol-(2) (febuprol) on the biliary tract is demonstrated in two different experimental arrangements in anesthetized dogs. This effect on the spasm provoked by morphine or prostigmine is illustrated by measuring the alteration of pressure in the choledochal duct. The spasmolytic efficacy of febuprol is significant and indicates a favourable secondary therapeutic effect of this substance.

1-Propanol↗
PubMed1978

Inhibition of bile salt excretion and bile flow by spasmolytic drugs. An additional therapeutic effect in the treatment of biliary colics?

The influence of the spasmolytic drugs hyoscin-N-butylbromide (HBB, Buscopan) and Extractum opii (E. opii) on bile flow, bile salt and bilirubin excretion is investigated in the cholecystectomized, unanaesthetized pig and compared with the results after acute, quantitative interruption of the enterohepatic circulation (EHC) by biliary drainage. The results demonstrate that HBB and E. opii induce a significant decrease in bile flow and bile salt excretion. A further analysis suggests that this effect is due to an inhibition of intestinal motility and transit time, followed by a delay of the EHC of bile salts with a decrease in biliary bile salt excretion and bile salt dependent bile flow. The results point out a second mechanism that might be responsible for the effectiveness of spasmolytic drugs in the treatment of biliary colics: the lowering of intraluminal pressure by inhibition of bile salt dependent bile flow.

Animals↗
PubMed1982

1,4-Benzodiazepines. VIII - Central depressive activity and spasmolytic action of isoquino-[2,1-d] [1,4] benzodiazepines. Structure-activity relationships.

The pharmacological activity of four new groups of isoquino [2,1-d] ((1,4]benzodiazepines, i.e. the 6-oxo-12,13-dimethoxy-5H-7H--9,10-dihydroisoquino [2,1-d] [1,4]benzodiazepinium bromides (I); 5,9,10,14b--tetrahydroisoquino [2,1-d] [1,4]benzodiazepin-7H-6-ones (II); 6-phenyl-12,13--dimethoxy-7,9,10,14b-tetrahydroisoquino [2,1-d] [1,4]benzodiazepines (III) and 6-phenyl-12,13-dimethoxy-7H-9,10-dihydroisoquino [2,1-d] [1,4]benzodiazepinium bromides (IV) was studied. All the compounds studied are biologically active. They show a depressive effect on the central nervous system, which is most pronounced in (II). It was established that the presence of alkyl substituents in the position-7 of the structure (II) as well as the chlorine atom in position-2 resulted in an increase of activity. Most of these compounds possess a mild or strong antinociceptive effect. Some of them exhibited an antireserpine activity as well. The spasmolytic effect of (IV) was strong while the rest of the compounds exerted a very weak spasmolytic effect. All the compounds tested on the autonomous nervous system possess the characteristics of weak sympathomimetics.

Animals↗
PubMed1994

Quercetin glycosides in Psidium guajava L. leaves and determination of a spasmolytic principle.

The traditional herbal remedy from Psidium guajava leaves has been medically proposed in Mexico as effective treatment of acute diarrhea. A methanolic leaf extract was subjected to a bioassay-guided isolation of spasmolytic constituents. Six fractions were separated on a polyvinylpolypyrrolidine (PVPP) column using a water methanol-gradient. The fraction containing flavonols inhibited peristalsis of guinea pig ileum in vitro. A trace of quercetin aglycone together with five glycosides was isolated from this active fraction and identified as quercetin 3-O-alpha-L-arabinoside (guajavarin); quercetin 3-O-beta-D-glucoside (isoquercetin); quercetin 3-O-beta-D-galactoside (hyperin); quercetin 3-O-beta-L-rhamnoside (quercitrin) and quercetin 3-O-gentobioside. Biological activity of each pure compound was studied in the same bioassay. Obtained results suggest that the spasmolytic activity of the Psidium guajava leaf remedy is mainly due to the aglycone quercetin, present in the leaf and in the extract mainly in the form of five flavonols, and whose effect is produced when these products are hydrolyzed by gastrointestinal fluid.

Animals↗
PubMed1994

Calcium-antagonist effect of quercetin and its relation with the spasmolytic properties of Psidium guajava L.

The antidiarrheal properties of water and methanolic extracts of Psidium guajava leaves have been demonstrated with anteriority and their spasmolytic effect was attributed to quercetin, a flavonoid contained in this plant. The present paper reports the intestinal smooth muscle relaxation produced by quercetin on isolated guinea pig ileum previously contracted by a depolarizing KCl solution. Quercetin also inhibited intestinal contraction induced by different concentrations of calcium, shifting the contraction curve to the right showing a clear calcium-antagonistic effect. Quercetin effect on ileal and aortic smooth muscles are compared, the ileum being more sensitive to this flavonoid. The calcium-antagonist property of quercetin is discussed and also its contribution to explain the spasmolytic effect of this popular herbal remedy.

Animals↗
PubMed1998

Comparison of the effects of various spasmolytic drugs on isolated human and porcine detrusor smooth muscle.

The spasmolytic activity of flavoxate (CAS 15301-69-6), anticholinergic agents oxybutynin (CAS 5633-20-5), and trospium chloride (CAS 10405-02-4), drugs commonly utilized in the therapy of hyperactive bladder, and phosphodiesterase (PDE) inhibitors papaverine (CAS 58-74-2) and vinpocetine (CAS 42971-09-5) on muscarinic contractions of detrusor smooth muscle strips isolated from human and porcine urinary bladder was studied in vitro using the organ bath technique. Trospium chloride was most effective in relaxing contractions elicited by muscarinic stimulation, while flavoxate was significantly less effective than all other drugs tested. The relaxing potency of oxybutynin was greater than those of PDE-inhibitors papaverine and vinpocetine but 3,000 fold less significant than those of trospium chloride. The effects of the individual drugs on muscarinic tension of both human and porcine detrusor muscle strips were nearly equal. The present results suggest that the pig might be an appropriate animal model for the study of effects of spasmolytic substances on the contractility of urinary bladder smooth muscle in vitro.

Animals↗
PubMed1976

[Animal experimental study on spasmolytic and analgesic activities of pramiverine, metamizole and their combination (author's transl)].

In two pharmacological in vivo tests a comparative study was performed on the spasmolytic and analgesic effects of 4,4-diphenyl-N-isopropyl-cyclohexylamine-hydrochloride (pramiverine, Sistalgin), metamizole and a combination of both active principles in equal dose ratio (1 : 1000). The results demonstrated that pramiverine showed a potent spasmolytic effect which was potentiated by the combination with metamizole, and that the positive analgesic effect of metamizole was fully displayed in the combination with pramiverine, but that for pramiverine alone no analgesic effect was detected.

Aminopyrine↗
PubMed1997

Intestinal trefoil factor (TFF 3) and pS2 (TFF 1), but not spasmolytic polypeptide (TFF 2) mRNAs are co-expressed in normal, hyperplastic, and neoplastic human breast epithelium.

pS2-TFF 1 is expressed in breast cancers and has been investigated as a potential prognostic factor reflecting oestrogen dependence. The relationship to the expression of other trefoil peptides, human spasmolytic polypeptide (hSP-TFF 2) and intestinal trefoil factor (hITF/hPI.B-TFF 3) is documented here. Fifty-seven breast specimens were selected from surgical pathology archives and included five normal breasts (two lactating), seven benign proliferative lesions, 11 ductal carcinomas in situ (DCIS), three lobular carcinomas in situ (LCIS), 24 invasive ductal carcinomas (IDC), and seven invasive lobular carcinomas (ILC). The comparative distribution of trefoil mRNAs was assessed by in situ hybridization using 35S-labelled riboprobes and immunohistochemical staining for pS2-TFF 1 and hSP-TFF 2. pS2-TFF 1 and hITF/hPI.B-TFF 3 mRNA were focally present at low signal intensity in normal and benign breast. Both pS2-TFF 1 and hITF/hPI.B-TFF 3 were expressed in all DCIS, LCIS and ILC, and 21/24 IDC. Overall, expression patterns of pS2-TFF 1 and hITF/hPI.B-TFF 3 coincided, but hITF/hPI.B-TFF 3 mRNA was usually found in a greater proportion of cells. Expression of hSP-TFF 2 peptide or mRNA was not detected in any of these cases. MCF 7 breast carcinoma cells also expressed hITF/hPI.B-TFF 3 and pS2-TFF 1 mRNAs but not hSP-TFF 2. hITF/hPI.B-TFF 3 co-expression with pS2-TFF 1 may act as a prognostic factor, but also raises questions about the regulatory pathway for pS2-TFF 1 hITF/hPI.B-TFF 3. Trefoil factors have effects on cell motility and spreading in vitro, and co-expression of hITF/hPI.B-TFF 3 with pS2-TFF 1 could be functionally significant if they form a heterodimer or compete for receptor binding. Absence of hSP-TFF 2 expression may be of equal relevance to tumour cell biology.

Blotting, Northern↗
PubMed1993

The expression of the trefoil peptides pS2 and human spasmolytic polypeptide (hSP) in 'gastric metaplasia' of the proximal duodenum: implications for the nature of 'gastric metaplasia'.

Expression of pS2 protein (an oestrogen-induced gene discovered in the MCF-7 breast carcinoma cell line) and its homologue human spasmolytic polypeptide (hSP) was analysed, using immunohistochemistry and in situ hybridization to their mRNAs, in the proximal duodenum of 17 partial gastrectomy specimens removed from individuals with chronic peptic ulceration. Eight were found to have gastric-type metaplasia. In gastric metaplasia, mRNAs for pS2 and hSP, and pS2 peptide antibody were co-localized in the cells covering the duodenal villi. pS2 immunostaining was diffusely cytoplasmic in nature. A similar pattern was seen in Brunner's gland ducts. The trefoil peptide localization in gastric metaplasia closely resembles that seen in superficial gastric epithelium and the distal Brunner's gland duct, which in turn shares morphological similarities with gastric epithelium. We therefore conclude that gastric metaplasia may be the result of an expansion of the surface component of the Brunner's gland duct. The function of these trefoil peptides is at present unknown, but their distribution elsewhere suggests an involvement in reparative mechanisms. The similarities between gastric foveolar and Brunner's gland duct epithelium may derive from common restitution-enhancing features pertinent to a locally harsh environment.

Brunner Glands↗
PubMed1994

Expression of the trefoil peptides pS2 and human spasmolytic polypeptide (hSP) in Barrett's metaplasia and the native oesophageal epithelium: delineation of epithelial phenotype.

The distribution of the two trefoil peptides pS2 and human spasmolytic polypeptide (hSP) and their mRNAs was investigated in 90 selected oesophageal biopsies, 23 of which contained epithelium with wholly gastric cardiac-type morphology, 52 specialized (intestinal)-type metaplasia, and 15 non-metaplastic oesophageal epithelium. No fundic-type epithelium was represented. The cardiac-type epithelium resembled true gastric antral epithelium, with hSP and pS2 mRNA localization to the superficial/foveolar compartment and hSP mRNA alone in deeper glands. The pattern of peptide distribution was broadly in line with the mRNA, but hSP peptide was generally not demonstrable in the surface epithelium. pS2 immunostaining was diffusely cytoplasmic, whereas in specialized-type mucosa it was aggregated and cytoplasmic. hSP mRNA was demonstrable in surface epithelium of incomplete- but not complete-type intestinal (specialized) metaplasia. Deep glands with morphological features of pyloric glands/ulcer-associated cell lineage (UACL) typically contained only hSP peptide and its mRNA. In three biopsies containing specialized epithelium, small foci morphologically identical to true small intestinal surface epithelium were seen in which only pS2 mRNA and peptide were found and then only in rare goblet cells. Neither squamous epithelium nor oesophageal glands contained demonstrable pS2/hSP mRNA or peptide. The function of these proteins in the metaplastic mucosa of Barrett's oesophagus is unknown but they may reflect an epithelium responding to repeated insult. Their localization facilitates definition of the disparate epithelium types seen in this portion of the gut, with both native gastric and intestinal epithelia, and may help to pinpoint high-risk epithelium in Barrett's oesophagus, a potentially preneoplastic condition.

Barrett Esophagus↗
PubMed1995

Experimental ulceration leads to sequential expression of spasmolytic polypeptide, intestinal trefoil factor, epidermal growth factor and transforming growth factor alpha mRNAs in rat stomach.

A model of gastric ulceration in the rat has been used to determine the expression of four messenger RNAs (mRNAs) encoding peptides considered to play active parts in the healing response. The trefoil peptides, rat spasmolytic polypeptide (rSP) and rat intestinal trefoil factor (rITF), along with epidermal growth factor (EGF) and transforming growth factor alpha (TGF alpha) were the molecules studied. Ulceration was caused under anaesthesia by brief application of a liquid nitrogen-filled cryoprobe to the gastric serosal surface and RNA expression was monitored over the next 10 days. Each mRNA was quantified by ribonuclease protection assay, and mRNAs encoding rSP and rITF were localized within tissue sections by hybridization in situ with 35S antisense riboprobes. Ulceration induced the very rapid expression of first rSP and then rITF mRNA, whereas the mRNAs encoding EGF and TGF alpha increased at later times, with maxima recorded at 3 and 6 days, respectively. Hybridization in situ detected extensive rSP mRNA expression in the regenerative epithelia. The pronounced, but temporally different patterns of mRNA induction after ulceration suggest that the trefoil peptides may fulfil different and more immediate roles than the more 'traditional' healing proteins EGF and TGF alpha.

Animals↗
PubMed1992

Pancreatic spasmolytic polypeptide: crystallization, circular dichroism analysis, and preliminary X-ray diffraction studies.

Pancreatic spasmolytic polypeptide (PSP) isolated from porcine pancreas has been crystallized by the hanging drop vapor diffusion method. Crystals suitable for X-ray diffraction analysis were grown at pH 4.7 from a solution of 6% saturated ammonium sulfate. The space group is orthorhombic I222 or I2(1)2(1)2(1) with unit cell parameters a = 54.38 A, b = 72.29 A, and c = 180.85 A. There are three molecules of PSP per asymmetric unit and a water content of 46.9%. The crystals diffracts to an estimated resolution of 2.7 A. The far-UV CD spectrum of PSP shows some exceptional features which cannot be accounted for thoroughly in terms of standard secondary structures commonly seen in protein CD spectroscopy. With this limitation, the secondary structure analysis predicts 15% alpha-helix, between 10 and 20% antiparallel beta-strand, 10% parallel beta-strand, 15% turn, and 25 to 40% of other structures.

Amino Acid Sequence↗