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L Giudici

Publications and source records attributed to L Giudici.

10 recordsLinked to original sources
PubMed1994

Himbacine discriminates between putative muscarinic M1 receptor-mediated responses.

This study describes the antagonistic properties of himbacine, in comparison with those of pirenzepine, at muscarinic receptors mediating the depolarization of rat superior cervical ganglion, the inhibition of electrically-induced twitch contractions of rabbit vas deferens and the contraction of dog saphenous vein, currently classified as putative muscarinic M1 sites. The affinity of himbacine for the vas deferens site (pA2 8.08) was nearly ten times higher than those for the M1 receptors of rat ganglion and dog saphenous vein (pA2 7.14 and 7.16, respectively); affinity estimates for pirenzepine were similar throughout the different preparations. The present data are consistent with the allocation of ganglion and saphenous vein receptors into the M1 subclass; the profile of the vas deferens site, conversely, appears to be different, and possibly more closely related to that reported for the M4/m4 receptor.

(4-(m-Chlorophenylcarbamoyloxy)-2-butynyl)trimethy↗
PubMed1992

DAU 6285: a novel antagonist at the putative 5-HT4 receptor.

The antagonistic properties of DAU 6285, an azabicycloalkyl benzimidazolone derivative, at putative 5-hydroxytryptamine4 (5-HT4) receptors were investigated in in vitro preparations of guinea-pig ileum and human atrium, in comparison to ICS 205-930. DAU 6285 behaved as a competitive antagonist in all the preparations examined. Its affinity (pA2) ranged between 6.50 and 7.12 in the test models considered. The affinity of ICS 205-930 was 2-3 fold lower. At variance with ICS 205-930, DAU 6285 displayed a weak affinity for 5-HT3 receptors (pKi = 6.1, rat cortex; pA2 less than 5, guinea-pig ileum). In the guinea-pig ileum, DAU 6285 (10 microM) did not exert antimuscarinic, antihistaminic, antinicotinic or myolytic activity. Moreover, it did not bind to other 5-HT receptor subtypes, or to adrenergic, dopaminergic, benzodiazepine, nicotine, GABA receptors. DAU 6285 may represent a suitable tool for studies in the field of 5-HT4 receptors.

Animals↗
PubMed1991

[Transrectal echographic micturitional evaluation of bladder neck pathology].

Dynamic transrectal echography is the primary method to evaluate bladder neck diseases during micturition for its safety, noninvasiveness and excellent imaging. In order to find some features for every kind of disease, we have examined 32 patients with BPH, Carcinoma, Marion disease and also evaluated the morphological images after prostate surgery. Enlargement of the prostate gland may restrict the urethral lumen and deviate its intra-prostate way, such that the urethra can't be allocated in one sagittal echographic plane. The third lobe, when it exists, can act like a valve against the urine flow. Prostate carcinoma, at first, can be asymptomatic on urodynamic study. Urethral invasion and its organic stenosis is shown by a very thin, longer and irregular profiles. Bladder neck sclerosis is an unusual disease, but its diagnosis can be easy if a posterior "beak" at internal meatus level, urethral dilatation after stenosis and positive Stop-Test exist. After surgery, one can observe full relaxation of the internal sphincter and the voluntary skeletal sphincter, located at the level of the membranous urethra, providing itself a continence mechanism.

Carcinoma↗
PubMed1990

Affinity profile of the novel muscarinic antagonist, guanylpirenzepine.

The study reports the functional affinity of an amidino derivative of pirenzepine, guanylpirenzepine, for muscarinic receptors mediating relaxation of rat duodenum, inhibition of rabbit vas deferens twitch contraction (both receptors previously classified as M1), guinea pig negative inotropism (M2) and ileal contraction (M3). Unlike pirenzepine, guanylpirenzepine discriminated between duodenum and vas deferens receptors, with a 30-fold greater affinity for the former subtype. The unique selectivity pattern of guanylpirenzepine (duodenum greater than vas deferens greater than ileum greater than atrium) renders it a promising tool for the classification of muscarinic receptor subtypes.

Animals↗
PubMed1990

4-DAMP analogues reveal heterogeneity of M1 muscarinic receptors.

The muscarinic receptors responsible for two effects elicited by McN-A-343, i.e. the relaxation of the rat duodenum and the inhibition of the twitch contraction of rabbit vas deferens, were investigated by use of derivatives of 4-diphenyl acetoxy-N-methyl piperidine methobromide (4-DAMP). Both receptors had been previously identified as M1 on the basis of the high affinity shown towards pirenzepine. Schild analysis of antagonism revealed that the affinities of 4-DAMP and three of its analogues in the rat duodenum were significantly different from those estimated in rabbit vas deferens. These data indicate that distinct receptor subtypes mediate duodenal relaxation and vas deferens inhibition of twitch contraction and suggest that receptors classified as M1 by means of pirenzepine affinity constitute a heterogeneous population.

(4-(m-Chlorophenylcarbamoyloxy)-2-butynyl)trimethy↗
PubMed1977

Pharmacology of halopredone acetate, a new topical antiinflammatory steroid.

The topical antiinflammatory activity of 17,21-bis(acetyloxy)-2-bromo-6beta,9-difluoro-11beta-hydroxypregna-1,4-diene-3,20-dione (halopredone acetate; Topicon) has been compared with those of other steroids in a few bioassays in animals. At variance with the reference compounds, halopredone acetate, which exhibited variable potency according to the assay used never displayed substantial systemic effects when locally applied. Even after subcutaneous administration this new steroid did not interfere with adrenal function, carbohydrate and protein metabolism or sodium and potassium excretion. On the basis of the results reported, halopredone acetate may be considered a steroid with potentially high topical antiinflammatory activity and good tolerability.

Administration, Topical↗