In vivo evidence of partial agonist activity exerted by purported 5-hydroxytryptamine antagonists

1979 ◽  
Vol 58 (4) ◽  
pp. 505-509 ◽  
Author(s):  
Francis C. Colpaert ◽  
Carlos J.E. Niemegeers ◽  
Paul A.J. Janssen
Keyword(s):  
Partial Agonist ◽  
Agonist Activity ◽  
Partial Agonist Activity

scholarly journals Partial agonist activity of R3(BΔ23–27)R/I5 at RXFP3 – Investigation of in vivo and in vitro pharmacology

2015 ◽  
Vol 747 ◽  
pp. 123-131 ◽  
Author(s):  
Lisbeth Kristensson ◽  
Gaëll Mayer ◽  
Karolina Ploj ◽  
Martina Wetterlund ◽  
Susanne Arlbrandt ◽  
...  
Keyword(s):  
Partial Agonist ◽  
Agonist Activity ◽  
Partial Agonist Activity ◽  
In Vitro Pharmacology

Effects of Partial Agonist Activity (PAA) on β1 and β2 Receptor Subtypes in-vivo

1991 ◽  
Vol 81 (s25) ◽  
pp. 9P-9P
Author(s):  
NM Wheeldon ◽  
DG McDevitt ◽  
BJ Lipworth
Keyword(s):  
Partial Agonist ◽  
Receptor Subtypes ◽  
Agonist Activity ◽  
Partial Agonist Activity

scholarly journals Transactivation Function-1-Mediated Partial Agonist Activity of Selective Estrogen Receptor Modulator Requires Homo-Dimerization of the Estrogen Receptor α Ligand Binding Domain

2019 ◽  
Vol 20 (15) ◽  
pp. 3718 ◽  
Author(s):  
Yukitomo Arao ◽  
Kenneth S. Korach
Keyword(s):  
Estrogen Receptor ◽  
Ligand Binding ◽  
Partial Agonist ◽  
Binding Domain ◽  
Ligand Binding Domain ◽  
Agonist Activity ◽  
Partial Agonist Activity

The isolation of estrogen receptor alpha (ERα) cDNA was successful around 30 years ago. The characteristics of ERα protein have been examined from various aspects, primarily through in vitro cell culture studies, but more recently using in vivo experimental models. There remains, however, some uncharacterized ERα functionalities. In particular, the mechanism of partial agonist activity of selective estrogen receptor modulators (SERMs) that involves control of the N-terminal transcription function of ERα, termed AF-1, is still an unsolved ERα functionality. We review the possible mechanism of SERM-dependent regulation of ERα AF-1-mediated transcriptional activity, which includes the role of helix 12 of ERα ligand binding domain (LBD) for SERM-dependent AF-1 regulation. In addition, we describe a specific portion of the LBD that associates with blocking AF-1 activity with an additional role of the F-domain in mediating SERM activity.

Ferulic acid alleviates abnormal behaviors in isolation-reared mice via 5-HT1A receptor partial agonist activity

2021 ◽  
Author(s):  
Ryota Araki ◽  
Akira Yasubuchi ◽  
Marina Ikegaya ◽  
Chihiro Hojo ◽  
Hayato Tachioka ◽  
...  
Keyword(s):  
Ferulic Acid ◽  
Partial Agonist ◽  
Agonist Activity ◽  
Partial Agonist Activity ◽  
Abnormal Behaviors

Characterization of aripiprazole partial agonist activity at human dopamine D3 receptors

2008 ◽  
Vol 597 (1-3) ◽  
pp. 27-33 ◽  
Author(s):  
Yoshihiro Tadori ◽  
Robert A. Forbes ◽  
Robert D. McQuade ◽  
Tetsuro Kikuchi
Keyword(s):  
Partial Agonist ◽  
Agonist Activity ◽  
Dopamine D3 Receptors ◽  
D3 Receptors ◽  
Partial Agonist Activity ◽  
Dopamine D3

Effect of Partial Agonist Activity on the Side Effects of β-Blockade in Patients with Chronic Stable Angina

Drugs ◽  
1989 ◽  
Vol 38 (Supplement 2) ◽  
pp. 39-44
Author(s):  
John Chambers ◽  
MeiLin Ong ◽  
Fawaz Akhras ◽  
George Adam ◽  
Graham Jackson
Keyword(s):  
Side Effects ◽  
Stable Angina ◽  
Partial Agonist ◽  
Chronic Stable Angina ◽  
Agonist Activity ◽  
Partial Agonist Activity

Partial agonist activity of celiprolol, a cardioselective β-antagonist

1991 ◽  
Vol 194 (1) ◽  
pp. 1-5 ◽  
Author(s):  
Seishi Ochi ◽  
Mikio Nakazawa ◽  
Takahito Kimura ◽  
Yoshito Nakagawa ◽  
Shoichi Imai
Keyword(s):  
Partial Agonist ◽  
Agonist Activity ◽  
Partial Agonist Activity
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