Biomedical subjects
Publications and source records attributed to M Palomba.
Forty amides, formamidines and trifluoromethylsulfonylamides bearing on the nitrogen a cyclohexyl residue, eventually 2-substituted, were prepared and tested for analgesic activity against a chemical stimulus. Good activity was exhibited by amides 9, 11 and 28, by formamidine 34, as well as by triflyamide 40. Eleven additional compounds exhibited a moderate activity.
The ontogeny of muscarinic cholinergic receptors has been studied in different regions of the human fetal brain. For a comparison, the same study has been carried out on newborn and premature brain. Regarding on the areas examined (frontal cortex, cerebellum, hippocampus, thalamus and basal ganglia) either an increase or a decrease of receptor density during gestation was observed. Thus, the ontogeny of the receptors follows a different pattern in areas which differ in function, cholinergic innervation and embryological origin. However, in all the regions the affinity of the binding site for the ligand [3H]quinuclidinyl benzilate [3H]QNB was very similar to that reported for muscarinic receptors from adult mammalian brain. Data obtained from agonist binding (acetylcholine and carbachol) revealed the presence of a high (H)- and a low-affinity binding site (L) from 10 weeks of gestation. The selective antagonist pirenzepine (PZ) also distinguished two different muscarinic receptor subtypes, which however had higher affinity than that seen in adult brain. In conclusion, during ontogeny, the muscarinic acetylcholine receptor shares some but not all of the pharmacological properties shown in the adult brain.
Heterogeneity of muscarinic cholinergic receptors was investigated in chick embryo retina throughout development and in chicks immediately after hatching. The presence of a homogeneous receptor population was evidenced by antagonist binding. The affinity of antagonists increased up to day 14 of incubation, when synaptogenesis occurs. After this stage, it remained substantially unchanged. The number of receptors increased in embryos until hatching. On the contrary, agonists, such as acetylcholine and carbachol, bound to two (high- and low-affinity) binding sites. Through development, the affinity of both significantly increased until day 14, further substantiating the hypothesis of a maturation of the receptor pattern which precedes synapse formation. Muscarinic cholinergic binding seems to identify 3 critical steps in retinal neuronal development. The first is between 7 and 9 days of incubation, the second when synaptogenesis occurs and the third after initiation of function.
Explore the source record for details and available documents.
Explore the source record for details and available documents.
Seventeen (un)substituted N-[4-(propyl)cyclohexyl]-amides (6a-h, 7a-h and 8) were synthesized and tested as anti-inflammatory and analgesic agents. The substituents on the aromatic ring were chosen in order to study the influence of electron-withdrawing or electron-donating residues, that change the electronic density on the aromatic moiety. The pharmacological results allow drawing some preliminary considerations on structure-activity relationships.
PURPOSE: Posterior capsule opacification (PCO) after intraocular lens (IOL) implantation has a multifactored pathogenesis. Capsulorhexis and capsular bag implantation of a one-piece, biconvex poly(methyl methacrylate) (PMMA) IOL are likely to reduce the PCO incidence. This study was performed to determine whether an ideal capsulorhexis size able to reduce PCO incidence exists. METHODS: A retrospective study of 107 patients who had extracapsular cataract extraction with capsulorhexis and capsular bag IOL implantation was carried out. The PCO site (central, paracentral, and peripheral) and degree (mild, moderate, and severe) were evaluated in relation to the capsulorhexis edge location relative to the IOL optic. Slitlamp biomicroscopy and photography and examination with a three-mirror Goldmann lens were performed. Patients were divided into three groups. Group 1: capsulorhexis free edge located on the IOL optic for 360 degrees; Group 2: capsulorhexis free edge located asymmetrically on and peripherally to the IOL optic; Group 3: capsulorhexis free edge located peripherally to IOL optic for 360 degrees. Each group was divided into two subgroups; one received polyHema IOLs and the second, PMMA IOLs. RESULTS: In Groups 1 and 2, the capsular transparency was higher than in Group 3 (P < .04). Central opacification percentage was lower in Group 1 than in Groups 2 and 3 (P < .04). No statistically significant differences between the polyHema and the PMMA subgroups were seen. CONCLUSIONS: Capsulorhexis with a slightly smaller diameter than the IOL optic appears to be better than a large-size capsulorhexis in reducing the incidence of PCO.
Explore the source record for details and available documents.
Explore the source record for details and available documents.