scholarly journals The 5-HT1A Receptor Full Agonist, 8-OH-DPAT Inhibits ACTH-Induced 5-HT2A Receptor Hyperfunction in Rats: Involvement of 5-HT1A Receptors in the DOI-Induced Wet-Dog Shakes in ACTH-Treated Rats

2007 ◽  
Vol 30 (1) ◽  
pp. 117-120 ◽  
Author(s):  
Yoshihisa Kitamura ◽  
Kouhei Kitagawa ◽  
Yoshika Fujitani ◽  
Kazuhiko Shibata ◽  
Hiroaki Araki ◽  
...  
Keyword(s):  
Full Agonist ◽  
Wet Dog Shakes

RXR Partial Agonist Produced by Side Chain Repositioning of Alkoxy RXR Full Agonist Retains Antitype 2 Diabetes Activity without the Adverse Effects

2014 ◽  
Vol 58 (2) ◽  
pp. 912-926 ◽  
Author(s):  
Kohei Kawata ◽  
Ken-ichi Morishita ◽  
Mariko Nakayama ◽  
Shoya Yamada ◽  
Toshiki Kobayashi ◽  
...  
Keyword(s):  
Adverse Effects ◽  
Partial Agonist ◽  
Side Chain ◽  
Full Agonist

BMS-196085: A potent and selective full agonist of the human β3 adrenergic receptor

2001 ◽  
Vol 11 (23) ◽  
pp. 3041-3044 ◽  
Author(s):  
A.V. Gavai ◽  
P.M. Sher ◽  
A.B. Mikkilineni ◽  
K.M. Poss ◽  
P.J. McCann ◽  
...  
Keyword(s):  
Adrenergic Receptor ◽  
Full Agonist

trans-2,3-Dihydroxy-6a,7,8,12b-tetrahydro-6H-chromeno[3,4-c]isoquinoline:  Synthesis, Resolution, and Preliminary Pharmacological Characterization of a New Dopamine D1Receptor Full Agonist

2006 ◽  
Vol 49 (23) ◽  
pp. 6848-6857 ◽  
Author(s):  
Juan Pablo Cueva ◽  
Gianfabio Giorgioni ◽  
Russell A. Grubbs ◽  
Benjamin R. Chemel ◽  
Val J. Watts ◽  
...  
Keyword(s):  
Pharmacological Characterization ◽  
Full Agonist

Abecarnil is a Full Agonist at Some, and a Partial Agonist at Other Recombinant GABAA Receptor Subtypes

1993 ◽  
pp. 50-61 ◽  
Author(s):  
I. Pribilla ◽  
R. Neuhaus ◽  
R. Huba ◽  
M. Hillmann ◽  
J. D. Turner ◽  
...  
Keyword(s):  
Gabaa Receptor ◽  
Partial Agonist ◽  
Receptor Subtypes ◽  
Full Agonist ◽  
Gabaa Receptor Subtypes

751-P: First-in-Human, Single and Repeated Dose Study of SCO-267, a GPR40 Full Agonist, in Healthy Adults and Subjects with Glucose Intolerance

Diabetes ◽  
2021 ◽  
Vol 70 (Supplement 1) ◽  
pp. 751-P
Author(s):  
HARUNOBU NISHIZAKI ◽  
OSAMU MATSUOKA ◽  
MEGURU ACHIRA ◽  
TOMOYA KAGAWA ◽  
MASANORI WATANABE ◽  
...  
Keyword(s):  
Glucose Intolerance ◽  
Healthy Adults ◽  
Repeated Dose ◽  
Full Agonist ◽  
Dose Study

scholarly journals In Silico Identification and Experimental Validation of (−)-Muqubilin A, a Marine Norterpene Peroxide, as PPARα/γ-RXRα Agonist and RARα Positive Allosteric Modulator

Marine Drugs ◽  
2019 ◽  
Vol 17 (2) ◽  
pp. 110 ◽  
Author(s):  
Enrico D’Aniello ◽  
Fabio Iannotti ◽  
Lauren Falkenberg ◽  
Andrea Martella ◽  
Alessandra Gentile ◽  
...  
Keyword(s):  
Binding Mode ◽  
Allosteric Modulator ◽  
Positive Allosteric Modulator ◽  
Full Agonist ◽  
Synergistic Enhancement ◽  
Pharmacological Targets ◽  
In Vivo Analysis ◽  
Dynamics Simulations ◽  
Micromolar Range

The nuclear receptors (NRs) RARα, RXRα, PPARα, and PPARγ represent promising pharmacological targets for the treatment of neurodegenerative diseases. In the search for molecules able to simultaneously target all the above-mentioned NRs, we screened an in-house developed molecular database using a ligand-based approach, identifying (−)-Muqubilin (Muq), a cyclic peroxide norterpene from a marine sponge, as a potential hit. The ability of this compound to stably and effectively bind these NRs was assessed by molecular docking and molecular dynamics simulations. Muq recapitulated all the main interactions of a canonical full agonist for RXRα and both PPARα and PPARγ, whereas the binding mode toward RARα showed peculiar features potentially impairing its activity as full agonist. Luciferase assays confirmed that Muq acts as a full agonist for RXRα, PPARα, and PPARγ with an activity in the low- to sub-micromolar range. On the other hand, in the case of RAR, a very weak agonist activity was observed in the micromolar range. Quite surprisingly, we found that Muq is a positive allosteric modulator for RARα, as both luciferase assays and in vivo analysis using a zebrafish transgenic retinoic acid (RA) reporter line showed that co-administration of Muq with RA produced a potent synergistic enhancement of RARα activation and RA signaling.

scholarly journals Design and Identification of a GPR40 Full Agonist (SCO-267) Possessing a 2-Carbamoylphenyl Piperidine Moiety

2020 ◽  
Vol 63 (18) ◽  
pp. 10352-10379
Author(s):  
Hideki Furukawa ◽  
Yasufumi Miyamoto ◽  
Yasuhiro Hirata ◽  
Koji Watanabe ◽  
Yuko Hitomi ◽  
...  
Keyword(s):  
Full Agonist
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