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D Dragović

Publications and source records attributed to D Dragović.

15 recordsLinked to original sources
PubMed1997

Synthesis of several substituted phenylpiperazines behaving as mixed D2/5HT1A ligands.

Twenty-two different compounds have been synthesized with the aim of creating new, mixed D2/5HT1A ligands. For this purpose 1-substituted phenylpiperazines attached by the N-4 nitrogen to dopaminergic pharmacophores of the 2-(5-benzimidazole)ethyl-, 2-(5-benztriazole)ethyl-, 2-[5-(benzimidazole-2-thione)]ethyl- and 2-[6-(1,4-dihydroquinoxaline-2,3-dione)]ethyl-type were selected according to known structure-affinity requirements of 1-arylpiperazines. All the new compounds were evaluated for in-vitro binding affinity at the dopamine (D1 and D2) and 5-HT1A receptors. Synaptosomal membranes prepared from fresh bovine caudate nuclei and hippocampi were used as a source of dopamine and 5-hydroxytryptamine receptors, respectively. [3H]SCH 23390 (D1 selective), [3H]spiperone (D2 selective) and 8-OH-[3H]DPAT (5-HT1A selective) were employed as the radio-ligands. None of the compounds expressed affinity for binding at D1 dopamine receptors. Compounds 3b and 4b were inactive 8-OH-[3H]DPAT competitors whereas 1b, 2b and 4b were inactive in the [3H]spiperone-binding assay. The other compounds tested showed fair (1c, 1e, 1f, 2c, 2f, 3b, 3c and 4c) to high (1a, 1d, 2a, 1d, 3a, 3d-3f, 4a, and 4d) affinity in the [3H]spiperone-binding assay, the most potent representative being 4-[2-(5-benzimidazole-2-thione)ethyl]-1-(2-methoxyphenyl)piperazine, 3a (Ki = 1.7 nM). In the 8-OH-[3H]DPAT-displacement assay compounds 1b, 1d, 1f, 2b, 2f and 3f behaved as moderate competitors and 1a, 1c, 1e, 2a, 2c, 2d, 3a, 3c-3e, 4a, 4c, 4d and 4f as rather strong competitors; 4-[2-(5-benztriazole)ethyl]-1-(2-methoxyphenyl)piperazine, 2a had the highest binding affinity at the 5-HT1A receptors (Ki = 2.6 nM). Because many antipsychotic and anxiolytic agents behave as mixed dopaminergic and serotonergic ligands, the high affinity of several of these new ligands for binding at both D2 and 5-HT1A receptors make them promising candidates deserving further pharmacological evaluation as antipsychotic or anxiolytic pharmaceuticals.

Animals↗
PubMed1996

Synthesis of N-n-propyl-N-(2-arylethyl)-5-(1H-benzimidazol-2-thione)-eth ylamines and related compounds as potential dopaminergic ligands.

Twelve different N-n-propyl-N-(2-arylethyl)-5-(1H-benzimidazol-2-thione)-ethy lamines and 12 related heterocyclic congeners were synthesized with the aim of creating new high affinity dopaminergic ligands. Upon thorough chemical analysis they were evaluated for their affinity towards the D-1 and the D-2 dopamine receptors (DAR) by in vitro binding assay using synaptosomal membranes of the bovine caudate nuclei and [3H]SCH 23390 (R (+)-7-chloro-8-hydroxy-3-methyl-1-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride) (D-1 selective) and [3H]spiperone (D-2 selective) as the radioligands. None of the synthesized compounds expressed affinity for the binding to the D-1 DAR Compounds 11e, 11j, 11l, 12b, 12d, 13a, 13d, 14a, and 14d were also inactive competitors of [3H] spiperone binding to the D-2 DAR. However, 1H-benzimidazol-2-thione derivatives 11k, 11h, and 11f and 1, 4-di-hydroquinoxalin-2,3-dione derivative 12c (in this rank order of potencies) acted as strong competitors of [3H] spiperone binding to the D-2 receptors under conditions that prevented radioligand binding to serotonin 5HT(2) receptors. Relationship between the structure and affinities of the new ligands for the binding to the D-2 DAR as well as the demands of the receptor itself for the interaction with the new compounds are discussed.

Animals↗
PubMed1995

Synthesis and evaluation of N,N-di-n-propyl-5,6,7,8-tetrahydro-1 H-benz[f]benzimidazol-6-yl-amine and related congeners as dopaminergic ligands.

Four semirigid dopaminergic biosiosteres (N,N-di-n-propyl-5,6,7,8-tetrahydro-1 H-benz[f]benzimidazol-6-yl-amine [sequence: see text] and three related congeners) were synthesized and chemically characterized. The affinity and selectivity of these compounds for D-1 and D-2 classes of the dopamine receptor were determined in competition binding experiments using synaptosomal membranes of the bovine caudate nuclei and [3H]SCH 23390 (D-1 selective) and [3H]spiperone (D-2 selective) as radioligands. None of the four compounds tested expressed significant affinity for D-1 receptors and all of them competed moderately with [3H]spiperone binding to D-2 receptors under conditions that prevented radioligand binding to serotonin 5HT2 receptors. Some aspects of structure affinity relationship for this class of dopaminergic ligands are discussed.

2-Naphthylamine↗
PubMedDate not supplied

[Indications for female sterilization in our surgical records].

During the period of 1970--1979 there were 303 patients sterilized by the Madlener method. Out of the them number. The highest number was delivered by caesarean section (182, 60%), and the highest number of the sterilized in the group of caesarean, section were multiparae with seven and more living children (102, 89.5%), then those with the third caesarean section (38, 76%), the fourth (3, 75%), the second (22, 10%), and the first caesarean section (17, 3.42%). Special conditions for sterilization were age, more than 30 years old, with three and more children with medical and socio-economic indications. In 21 women (40%) sterilization was performed as an additional intervention to the other laparatomies, when there was a special care about the number of living children (above three), age and medical indications. There were 3 (0,99%) failed sterilisations (one ectopic pregnancy and two in utero). The authors advocate women's free declaration for sterilization and respective legal acts.

Adult↗