Simultaneous blockade of 5-HT1A/B receptors and 5-HT transporters results in acute increases in extracellular 5-HT in both rats and guinea pigs: in vivo characterization of the novel 5-HT1A/B receptor antagonist/5-HT transport inhibitor SB-649915-B

2007 ◽  
Vol 192 (1) ◽  
pp. 121-133 ◽  
Author(s):  
Zoë A. Hughes ◽  
Kathryn R. Starr ◽  
Claire M. Scott ◽  
Michael J. Newson ◽  
Trevor Sharp ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Guinea Pigs ◽  
The Novel ◽  
Transport Inhibitor ◽  
In Vivo Characterization

In Vivo Characterization of the Novel Neuropeptide Y Y1 Receptor Antagonist H 409/22

2000 ◽  
Vol 36 (4) ◽  
pp. 516-525 ◽  
Author(s):  
Rickard E. Malmström ◽  
Andreas Alexandersson ◽  
Karin C. Balmér ◽  
Jessika Weilitz
Keyword(s):  
Neuropeptide Y ◽  
Receptor Antagonist ◽  
The Novel ◽  
Y1 Receptor ◽  
In Vivo Characterization

In vivo characterization of the putative 5-HT1A receptor antagonist SDZ 216,525 using two models of somatodendritic 5-HT1A receptor function

1994 ◽  
Vol 33 (3-4) ◽  
pp. 359-366 ◽  
Author(s):  
C. Routledge ◽  
J. Hartley ◽  
J. Gurling ◽  
M. Ashworth-Preece ◽  
G. Brown ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Receptor Function ◽  
In Vivo Characterization

scholarly journals In Vivo Characterization of a Novel -Secretase Inhibitor SCH 697466 in Rodents and Investigation of Strategies for Managing Notch-Related Side Effects

2013 ◽  
Vol 2013 ◽  
pp. 1-14 ◽  
Author(s):  
Lynn A. Hyde ◽  
Qi Zhang ◽  
Robert A. Del Vecchio ◽  
Prescott T. Leach ◽  
Mary E. Cohen-Williams ◽  
...  
Keyword(s):  
Side Effects ◽  
Repeated Administration ◽  
Therapeutic Benefit ◽  
The Novel ◽  
Substantial Evidence ◽  
Amyloid A ◽  
Secretase Inhibitor ◽  
In Vivo Characterization

Substantial evidence implicates -amyloid (A) peptides in the etiology of Alzheimer’s disease (AD). A is produced by the proteolytic cleavage of the amyloid precursor protein by - and -secretase suggesting that -secretase inhibition may provide therapeutic benefit for AD. Although many -secretase inhibitors have been shown to be potent at lowering A, some have also been shown to have side effects following repeated administration. All of these side effects can be attributed to altered Notch signaling, another -secretase substrate. Here we describe the in vivo characterization of the novel -secretase inhibitor SCH 697466 in rodents. Although SCH 697466 was effective at lowering A, Notch-related side effects in the intestine and thymus were observed following subchronic administration at doses that provided sustained and complete lowering of A. However, additional studies revealed that both partial but sustained lowering of Aand complete but less sustained lowering of A were successful approaches for managing Notch-related side effects. Further, changes in several Notch-related biomarkers paralleled the side effect observations. Taken together, these studies demonstrated that, by carefully varying the extent and duration of A lowering by -secretase inhibitors, it is possible to obtain robust and sustained lowering of A without evidence of Notch-related side effects.

scholarly journals In Vitro and In Vivo Characterization of the Non-peptide NK3 Receptor Antagonist SB-223412 (Talnetant): Potential Therapeutic Utility in the Treatment of Schizophrenia

2007 ◽  
Vol 33 (7) ◽  
pp. 1642-1652 ◽  
Author(s):  
Lee A Dawson ◽  
Katherine J Cato ◽  
Claire Scott ◽  
Jeannette M Watson ◽  
Martyn D Wood ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Nk3 Receptor ◽  
In Vivo Characterization ◽  
Therapeutic Utility

In vitro and in vivo characterization of the novel GABAB receptor positive allosteric modulator, 2-{1-[2-(4-chlorophenyl)-5-methylpyrazolo[1,5-a]pyrimidin-7-yl]-2-piperidinyl}ethanol (CMPPE)

2011 ◽  
Vol 61 (5-6) ◽  
pp. 957-966 ◽  
Author(s):  
Elisabetta Perdona’ ◽  
Vivian J.A. Costantini ◽  
Michela Tessari ◽  
Prisca Martinelli ◽  
Corrado Carignani ◽  
...  
Keyword(s):  
Gabab Receptor ◽  
Allosteric Modulator ◽  
The Novel ◽  
Positive Allosteric Modulator ◽  
In Vivo Characterization

scholarly journals In vitro and in vivo characterization of PF-04418948, a novel, potent and selective prostaglandin EP2 receptor antagonist

2011 ◽  
Vol 164 (7) ◽  
pp. 1847-1856 ◽  
Author(s):  
KJ af Forselles ◽  
J Root ◽  
T Clarke ◽  
D Davey ◽  
K Aughton ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Ep2 Receptor ◽  
In Vivo Characterization
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