Identification and in Vivo and in Vitro Characterization of Long Acting and Melanocortin 4 Receptor (MC4-R) Selective α-Melanocyte-Stimulating Hormone (α-MSH) Analogues

2012 ◽  
Vol 55 (5) ◽  
pp. 1969-1977 ◽  
Author(s):  
Kilian Conde-Frieboes ◽  
Henning Thøgersen ◽  
Jesper F. Lau ◽  
Ulrich Sensfuss ◽  
Thomas K. Hansen ◽  
...  
Keyword(s):  
Melanocyte Stimulating Hormone ◽  
Melanocortin 4 Receptor ◽  
In Vitro Characterization ◽  
Long Acting ◽  
Stimulating Hormone

Asymmetric synthesis and in vivo/in vitro characterization of new hybrid anticonvulsants derived from (2,5-dioxopyrrolidin-1-yl)phenylacetamides

2021 ◽  
Vol 109 ◽  
pp. 104751
Author(s):  
Michał Abram ◽  
Anna Rapacz ◽  
Gniewomir Latacz ◽  
Bartłomiej Szulczyk ◽  
Justyna Kalinowska-Tłuścik ◽  
...  
Keyword(s):  
Asymmetric Synthesis ◽  
In Vitro Characterization

scholarly journals In vivo and in vitro characterization of overproduced colicin E9 immunity protein

1992 ◽  
Vol 207 (2) ◽  
pp. 687-695 ◽  
Author(s):  
Russell WALLIS ◽  
Ann REILLY ◽  
Arthur ROWE ◽  
Geoffrey R. MOORE ◽  
Richard JAMES ◽  
...  
Keyword(s):  
Immunity Protein ◽  
In Vitro Characterization ◽  
Colicin E9

scholarly journals Identification of a Novel Delta Opioid Receptor Agonist Chemotype with Potential Negative Allosteric Modulator Capabilities

Molecules ◽  
2021 ◽  
Vol 26 (23) ◽  
pp. 7236
Author(s):  
Yazan J. Meqbil ◽  
Hongyu Su ◽  
Robert J. Cassell ◽  
Kendall L. Mores ◽  
Anna M. Gutridge ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Clinical Drug Development ◽  
In Vitro Characterization ◽  
Opioid Receptor Agonist ◽  
Negative Allosteric Modulator ◽  
Δ Opioid Receptor ◽  
Clinical Drug

The δ-opioid receptor (δOR) holds great potential as a therapeutic target. Yet, clinical drug development, which has focused on δOR agonists that mimic the potent and selective tool compound SNC80 have largely failed. It has increasingly become apparent that the SNC80 scaffold carries with it potent and efficacious β-arrestin recruitment. Here, we screened a relatively small (5120 molecules) physical drug library to identify δOR agonists that underrecruit β-arrestin, as it has been suggested that compounds that efficaciously recruit β-arrestin are proconvulsant. The screen identified a hit compound and further characterization using cellular binding and signaling assays revealed that this molecule (R995045, compound 1) exhibited ten-fold selectivity over µ- and κ-opioid receptors. Compound 1 represents a novel chemotype at the δOR. A subsequent characterization of fourteen analogs of compound 1, however did not identify a more potent δOR agonist. Computational modeling and in vitro characterization of compound 1 in the presence of the endogenous agonist leu-enkephalin suggest compound 1 may also bind allosterically and negatively modulate the potency of Leu-enkephalin to inhibit cAMP, acting as a ‘NAM-agonist’ in this assay. The potential physiological utility of such a class of compounds will need to be assessed in future in vivo assays.

In vivo and in vitro characterization of rifampicine suppositories

2009 ◽  
Vol 19 (3) ◽  
pp. 217-221
Author(s):  
H.M. El-Nahas ◽  
F.S. Ghazy ◽  
H.A. El-Ghamry ◽  
A.M. El-Wsaby
Keyword(s):  
In Vitro Characterization

In vivo and in vitro trimethadione oxidation activity of the liver from various animal species including mouse, hamster, rat, rabbit, dog, monkey and human

1999 ◽  
Vol 18 (1) ◽  
pp. 12-16 ◽  
Author(s):  
E Tanaka ◽  
A Ishikawa ◽  
T Horie
Keyword(s):  
Animal Species ◽  
In Vitro Study ◽  
Metabolic Clearance ◽  
Oxidation Activity ◽  
In Vitro Characterization ◽  
Demethylase Activity ◽  
Total Body

Trimethadione (TMO) has the properties required of a probe drug for the evaluation of hepatic drug-oxidizing capacity and, in this study, we have summarized the in vivo and in vitro metabolism of TMO in various animal species including mouse, hamster, rat, rabbit, dog, monkey and human. In the in vivo study, the plasma TMO level was measured after intravenous or oral (human) administration of TMO at a dose of 4 mg/kg to various animal species. The rate of TMO metabolic clearance in these animal species in vivo was in the order mouse > hamster >rat>rabbit>dog>monkey>human. In the in vitro study, species differences were observed in the cytochrome P450 (P450) content and drug-oxidizing enzyme activity. The content of P450 was monkey> mouse>dog>rabbit>hamster>rat>human. On the other hand, TMO N-demethylation was in the order mouse >hamster >rat >rabbit>dog>monkey>human. There was a good correlation between the mean total body clearance of TMO ( in vivo)andthemeanTMON-demethylase activity ( in vitro) (y=1.7×+0.11, r=0.965, P<0.001). These results show that TMO is a probe agent with metabolic and pharmacokinetic characteristics making it attractive for the in vivo and in vitro characterization of metabolic activity in various animal species.

In vitro characterization of PRRSV isolates with different in vivo virulence using monocyte-derived macrophages

2019 ◽  
Vol 231 ◽  
pp. 139-146 ◽  
Author(s):  
Giulia Ogno ◽  
Carmen A. Sautter ◽  
Elena Canelli ◽  
Obdulio García-Nicolás ◽  
Tomasz Stadejek ◽  
...  
Keyword(s):  
In Vitro Characterization
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