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PubMedDate not supplied

Effect of linking bridge modifications on the 5-HT1A receptor activity of some 4-(omega-benzotriazol-1-yl)alkyl-1-(2-methoxy-phenyl)piperazines.

A new series of arylpiperazines with two (2a-4a) and four (2c-4c) methylene spacers was synthesized. Compounds 2a, 2c, 3c, 4a and 4c were found to be 5-HT1A ligands (Ki = 4-88 nM). The most promising compound, 2c, bound with the highest affinity (Ki = 4 nM) at 5-HT1A sites. The results of in vivo experiments showed that compounds 2a-4a were inactive, while 2c-4c revealed a distinct antagonistic activity towards postsynaptic 5-HT1A receptors. The pharmacological profile of the tested compounds was discussed in comparison with that of the three methylene analogs b, described earlier.

8-Hydroxy-2-(di-n-propylamino)tetralin↗
PubMed2000

Selective inhibition of human cytochrome P450 3A4 by N-[2(R)-hydroxy-1(S)-indanyl]-5-[2(S)-(1, 1-dimethylethylaminocarbonyl)-4-[(furo[2, 3-b]pyridin-5-yl)methyl]piperazin-1-yl]-4(S)-hydroxy-2(R)-phenylmethy lpentanamide and P-glycoprotein by valspodar in gene transfectant systems.

Our previous report showed that L754.394 and valspodar (PSC833) are potent inhibitors of midazolam hydroxylation in human jejunum microsomes and vectorial transport of vinblastine in Caco-2 cells, respectively. In the present study, to directly examine the interactions of these compounds as well as other substrates with CYP3A4 and P-glycoprotein (P-gp), we performed in vitro inhibition studies using recombinant CYP3A4-expressed microsomes and an MDR1-transfected cell line, LLC-MDR1, respectively. In CYP3A4-expressed microsomes, both L754.394 and ketoconazole, at a concentration less than 0.5 microM, are the most potent inhibitors of the formation of 1'-hydroxymidazolam, a major metabolite of midazolam formed by CYP3A4. The greatest inhibitory effect on the transcellular transport of digoxin in LLC-MDR1 cells was observed in the presence of valspodar (<0.1 microM), followed by verapamil. From a comparison of the IC(50) values, it was shown that L754.394 and valspodar exhibited the highest selectivity for CYP3A4 and P-gp, respectively. To demonstrate such specificity, both midazolam hydroxylation and digoxin transport were observed in CYP3A4 transfected Caco-2 cells, which coexpress both P-gp and CYP3A4, in the presence or absence of L754.394 (0.5 microM) and valspodar (1.0 microM). L754.394 almost completely inhibited midazolam hydroxylation, but not digoxin transport, whereas almost complete inhibition of digoxin transport was observed in the presence of valspodar, but inhibition of the hydroxylation was minimal. Thus, the present study has demonstrated that L754.394 has a specific inhibitory effect on CYP3A4, whereas valspodar is specific for P-gp.

ATP Binding Cassette Transporter, Subfamily B, Mem↗
PubMed1975

[Bicyclic analogs of piperazine. XIII (1). Derivatives of 3,8-diazabicyclo[3.2.1]octane with potential anti-inflammatory activity].

The Authors describe the synthesis of some 8-acyl-3-methyl-3,8-diazabicyclo[3.2.1]octanes and 3-acyl-8-methyl-3,8-diazabicylo[3.2.1] octanes. The compounds were prepared by acylation of the corresponding methyl derivatives with the purpose of obtaining antiinflammatory compounds. The synthesis of some 3-alkyl-8-propionyl-3,8-diazabicylo[3.2.1]octanes is also described. These compounds were prepared in analogy with some 8-pripionyl-3,8-diazabicyclo[3.2.1]octanes endowed with high analgesic and antiinflammatory activity.

Anti-Inflammatory Agents↗
PubMed1975

[Spasmolytic activity of a piperazine derivative under the code number of 4P-79].

The author examined the pharmacologic spasmolytic action of a pyperasine derivative under the code 4P-79. She examined the effect of the compound on four types of spasms, induced by acethylcholine, nicotine, histamine and serotonine on an isolated rabbit intestine. The mean effective concentrations were determined and they were compared with the mean effective concentrations of papaverine and benzylharmine, estimated in parallel experiments. It was found that 4P-79 had high spasmolytic activity, surpassing several times that of the preparations used for comparison. There was a marked antiserotonine effect on the first place. The compound was examined also on an intestine "in situ" by the method of Nikolaev Comparative experiments with papaverine and deseryl were conducted.

Acetylcholine↗
PubMed2002

C-mycprotein expression upregulated by 2-(3-estrone-N-ethyl piperazine-methyl) tetracycline in bone.

AIM: To study the effect of XW630 on expression of pro-oncogene c-myc in the long bones of fetal mice in vitro for postulating the mechanism by which XW630 exerts its effect on bone. METHODS: The fetuses of pregnant mice were removed on day 16 of gestation, the long bones of the forelimbs of female fetal mice were freed of muscle and soft tissue and cultured in a specific device for 48 h in BGJb medium treated with 1 x 10(-7), 1 x 10(-8) and 1 x 10(-9) mol.L-1 XW630 in the final medium. After cultured for 48 h, the long bones were harvested and immunohistochemical analysis was performed for determination of c-Myc protein expression in epiphyseal plates. The areas of positive cells in the resting zone, proliferative zone and hypertrophic zone in epiphyseal plate were determined under image analytic system. RESULTS: When the concentration of XW630 in the medium was 1 x 10(-9) mol.L-1, the area of c-Myc positive cells increased in the proliferative zone compared with 1 x 10(-9) mol.L-1 in the estrone group, significant increase was also observed in the resting zone compared with the control group. When the concentration of XW630 in medium was 1 x 10(-8) or 1 x 10(-7) mol.L-1, stronger expression than that in the control group and the estrone group at the same concentration was observed in each of the three zones. CONCLUSION: The estrogenic effect of XW630 on bone was stronger than that of estrone. XW630 may promote proliferation and differentiation of chondroncytes by promoting c-Myc protein expression in chondroncytes. Thus, endochondral bone formation was enhanced.

Animals↗