Further Structure–Activity Relationships Study of Hybrid 7-{[2-(4-Phenylpiperazin-1-yl)ethyl]propylamino}-5,6,7,8-tetrahydronaphthalen-2-ol Analogues: Identification of a High-Affinity D3-Preferring Agonist with Potent in Vivo Activity with Long Duration of Action

2008 ◽  
Vol 51 (1) ◽  
pp. 101-117 ◽  
Author(s):  
Swati Biswas ◽  
Suhong Zhang ◽  
Fernando Fernandez ◽  
Balaram Ghosh ◽  
Juan Zhen ◽  
...  
Keyword(s):  
Duration Of Action ◽  
Structure Activity Relationships ◽  
High Affinity ◽  
Structure Activity ◽  
Long Duration

scholarly journals Measurement of the dynamics of stimulation and inhibition of steroidogenesis in isolated rat adrenal cells by using column perfusion

1974 ◽  
Vol 142 (2) ◽  
pp. 287-294 ◽  
Author(s):  
P. J. Lowry ◽  
Colin McMartin
Keyword(s):  
Cyclic Amp ◽  
Time Course ◽  
Acth Stimulation ◽  
Duration Of Action ◽  
Adrenal Cells ◽  
Small Column ◽  
Long Duration ◽  
Full Effect ◽  
Rapid Fall

Isolated adrenal cells were perfused in a small column by using Bio-Gel polyacrylamide beads as an inert supporting matrix, and the time-course of the response to various stimuli was observed by measuring fluorogenic 11-hydroxycorticosteroids in the effluent. A small but significant response was observed 1 min after stimulation with physiological concentrations of ACTH (adrenocorticotrophin), but the response did not start to build up rapidly for 3–4min and eventually reached a plateau after 9–10min. A similar pattern of events was observed for the decay of the steroid output on removal of ACTH. ACTH analogues, including one with a long duration of action in vivo, were found to produce responses with similar kinetics. However, cyclic AMP caused a more rapid increase in steroidogenesis and its effects were more short-lived after withdrawal. If, as present evidence suggests, cyclic AMP is produced rapidly after ACTH stimulation the delayed build-up of the steroidogenic response to ACTH would indicate that cyclic AMP may not be the intracellular mediator. When inhibitors were applied during ACTH stimulation, aminoglutethimide, which blocks mitochondrial conversion of cholesterol into pregnenolone (3β-hydroxypregn-5-en-20-one), caused a rapid fall in steroid output (1 min), whereas cycloheximide took longer to achieve its full effect. Nevertheless, the response had fallen by 50% in 2 min, indicating a much shorter half-life than that previously reported for the labile protein implicated in steroidogenesis. In addition the rapid response to cyclic AMP makes it unlikely that steroid production is induced as a result of initiation of protein synthesis. This suggests that the labile protein plays an obligatory but permissive role in the development of the response. Column perfusion has proved to be a simple technique which can readily yield accurate data on responses of cells to stimulants and inhibitors.

ChemInform Abstract: Structure-Activity Relationships of 1,3-Benzoxazole-4-carbonitriles as Novel Antifungal Agents with Potent in vivo Efficacy.

ChemInform ◽  
2011 ◽  
Vol 42 (35) ◽  
pp. no-no
Author(s):  
Jun-ichi Kuroyanagi ◽  
Kazuo Kanai ◽  
Takao Horiuchi ◽  
Hiroshi Takeshita ◽  
Shozo Kobayashi ◽  
...  
Keyword(s):  
Antifungal Agents ◽  
In Vivo Efficacy ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Abstract Structure

In Vivo and in Vitro Structure-Activity Relationships and Structural Conformation of Kisspeptin-10-Related Peptides

2009 ◽  
Vol 76 (1) ◽  
pp. 58-67 ◽  
Author(s):  
Ester Gutiérrez-Pascual ◽  
Jérôme Leprince ◽  
Antonio J. Martínez-Fuentes ◽  
Isabelle Ségalas-Milazzo ◽  
Rafael Pineda ◽  
...  
Keyword(s):  
Structure Activity Relationships ◽  
Structural Conformation ◽  
Structure Activity

Quantitative Structure Activity Relationships of Fungicidally Active Triazoles: Analogs and Stereoisomers of Propiconazole and Etaconazole Quantitative Structure Activity Relationships of Fungicidally Active Triazoles: Analogs and Stereoisomers of Propiconazole and Etaconazole

1989 ◽  
Vol 44 (1-2) ◽  
pp. 85-96 ◽  
Author(s):  
E. Ebert ◽  
W. Eckhardt ◽  
K. Jäkel ◽  
D. Sozzi ◽  
C. Vogel ◽  
...  
Keyword(s):  
Fungicidal Activity ◽  
Quantitative Structure ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Quantitative Structure Activity Relationships

Abstract The preparation of the four stereoisomers of propiconazole (TILT®) is described. Their inhibition of the 14α-C-demethylation of the sterol nucleus is examined and compared with the inhibition by the four stereoisomers of etaconazole (SONAX®). The quantitative structure-activity relationships (QSAR) of substituted 1,3-dioxolane-2-yl-methyltriazoles and 1,3-dioxane-2-ylmethyltriazoles on in vivo fungicidal activity are investigated.

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