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The lyophilized aqueous extracts from Cistus incanus L. (CI) and Cistus monspeliensis L. (CM) collected in Sicily were studied in order to evaluate their myorelaxant activity by using isolated smooth muscle of rat ileum and rat aorta. Both CI and CM extracts concentration-dependently inhibited the contractile response to acetylcholine (ACh), phenylephrine (PE) and to 100 mM KCl. The concentration-contraction curves to ACh in ileum and to PE in aorta, were displaced to the right by Cistus extracts in a non-competitive manner, with a depression of the maximum contractile response. The EC50 (microg/ml) of CM and CI were: ileum/KCl, CM 457+/-99, CI 681+/-80; ileum/ACh 100 microM, CM 297+/-66, CI 335+/-41; aorta/KCl, CM 360+/-21, CI 843+/-36; and aorta/PE 10 microM, CM 287+/-33, CI 451+/-58. The two extracts resulted almost equi-active in ileum, whereas CM was more active than CI in aorta. These data indicate that Cistus extracts act as spasmolytic on intestinal and vascular smooth muscle. The antagonism they exert on ACh-, PE- and KCl-evoked contractions seems to be functional, because it is not specifically directed toward any particular receptor; furthermore, a calcium-antagonist activity seems unlikely, since the extracts are capable of completely block the contractile response to agonists.

The antiulcer activity of a short-boiled aqueous extract from aerial parts of Cistus incanus was studied in rats against gastric lesions induced by necrotizing agents (1N HCl and absolute ethanol), indomethacin, serotonin and reserpine. The extract, containing bioflavonoids, was orally administered in the range from 0.25 to 0.50 g kg-1. It was found to have significant dose-related protective effects in all these experimental models, and was more effective against reserpine- and serotonin-induced mucosal congestion and haemorrhagic ulcers. These data suggest that the active constituents of the crude extract could be responsible for its protective effect by maintaining an efficient gastric mucosal microvascular supply.

In this study the pharmacological evaluation of MED-15, a non-acidic prodrug of tolmetin, is described. After oral administration the new compound shows a marked anti-inflammatory activity similar to that of tolmetin, but with minor ulcerogenic action and lower acute toxicity.

In the outline of the investigations concerning the analgesic and antiinflammatory activity of new fused heterocyclic compounds containing the pyrimidine ring, a series of 6H-thiazolo[3',2': 1,2]-5-oxopyrimido[5,4-b]indole derivatives was synthesized. Pharmacological results are reported and discussed.

As a part of a study on analgesic and antiinflammatory active condensed heterocyclic compounds containing the pyrimidinic ring, a number of 6H-1,3,4-thiadiazolo [3',2':1,2]-5-oxopyrimido [5,4-b]indole and 1-phenyl-6H-1,2,4-triazolo [1',5':1,2]-5-oxopyrimido [5,4-b] indole were synthesized and tested. The results of pharmacological assays are reported and discussed.

Summary Rat epididymal adipose tissue artery releases, during incubation, a PGI 2 -like substance which is active on rat blood pressure as well on aggregation induced by collagen or ADP. The radioimmunoassay of 6-keto PGF 1α , the stable metabolite of PGI 2 , confirms that this eicosanoid is sinthesized also within the blood vessel cells supplying the adipocytes.