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Biomedical subjects

G Ostermann

Publications and source records attributed to G Ostermann.

80 records · Page 5Linked to original sources
PubMedDate not supplied

Further investigations on the alpha 1-adrenoceptor blocking properties of AR-C 239 in rats.

AR-C 239, a new alpha-adrenoceptor blocking drug, appears to act selectively on alpha 1 sites in rats. At peripheral sites, this drug did not change the tachycardia induced by spinal sympathetic outflow stimulation in pithed rats, and did not antagonize the inhibitory effects of clonidine on this preparation. In addition, AR-C 239 showed predominant alpha 1-adrenoceptor blocking properties in the bisected rat vas deferens preparation. AR-C 239 did not prevent or reverse the centrally mediated hypotensive and bradycardic actions induced by clonidine, in intact animals. In conclusion, AR-C 239 seems to be a very useful tool for the characterization of peripheral and central alpha 1-adrenoceptors, in this animal species.

Adrenergic alpha-Antagonists↗
PubMedDate not supplied

PAF-agonistic and -antagonistic behaviour of new synthetic ether phospholipids. II. Relationships between chemical structure and inhibition of PAF-induced human platelet activation.

A series of 30 newly synthesised racemic ether phospholipids was evaluated for PAF-antagonistic action on human blood platelets in vitro. The chemical structure of these compounds was derived from the 1-O-hexadecyl-2-O-ethyl-glycero-3-phosphoric acid 4-(N,N-dimethylamino)pyridinium ethylester which was recently characterised as a PAF-specific antagonist. Anti-PAF effects were demonstrated by means of an aggregation and a binding assay. The inhibition was concentration-dependent and of competitive type. KB-values for inhibiting platelet aggregation in plasma were greater than or equal to 0.3 mumol/l. The most effective antagonists were 3-10 times more effective in comparison with the ginkgolide BN 52021. Structure-activity relationship studies showed the 4-dimethylaminopyridine moiety in the 3 position to be the ultimate structural requirement for expressing PAF-antagonistic activity. Moreover, a short-chain substituent in the 2 position and a distinct distance between the phosphate group and the onium center were found to be essential for high PAF-antagonistic activity.

Blood Platelets↗
PubMedDate not supplied

PAF-agonistic and -antagonistic behaviour of new synthetic ether phospholipids. I. Studies on blood platelets in vitro.

Structural analogues of platelet-activating factor (PAF, 1-O-alkyl-2-O-acetyl-sn-glycero-3-phosphocholine) in which the acetyl group and the polar head have been replaced by ethyl and a pyridine ring, respectively, were tested for biological activities on blood platelets in vitro. In comparison with PAF most of the analogues exerted weak pro-aggregatory effects and both structural modifications were found to contribute to the lowering of platelet-stimulating activity. 1-O-Hexadecyl-2-O-ethyl-rac-glycero-3-phosphoric acid 4-(N,N-dimethylamino)-pyridinium ethylester (DMAP-ethyl-PAF) did not activate platelets but inhibited PAF-induced platelet responses. The inhibition was concentration-dependent and of competitive type. KB values for inhibiting the PAF-induced aggregation of human and rabbit platelets in plasma were 3.2 and 0.55 mumol/l, respectively. There is also evidence that the PAF-antagonistic behaviour of DMAP-ethyl-PAF is attributable to an inhibition of the binding of PAF to its putative receptor.

Humans↗
PubMedDate not supplied

[Insulin-requiring diabetes].

The insulinorequiring diabetes is a notion which deserves a clear definition, essentially clinical, because it covers a wide range of physiopathological situations. The progressive degradation of Diabetes type II means a progressive discrepancy of insulinosecretion and above all an increase of insulinoresistance. The noxious part of chronical hyperglycemia is at present well known. The present therapeutical prospects tend to delay or limit insulinotherapy, by trying to obtain remission of insulinorequiring and some attempt to give a combined treatment associating insulin and hypoglycemic drugs.

Diabetes Mellitus, Type 1↗