A DFT approach to discriminate the antagonist and partial agonist activity of ligands binding to the NMDA receptor

2017 ◽  
Vol 116 (3) ◽  
pp. 323-337
Author(s):  
Zeynep Pinar Haslak ◽  
Esra Bozkurt ◽  
Bercem Dutagaci ◽  
Frank De Proft ◽  
Viktorya Aviyente ◽  
...  
Keyword(s):  
Nmda Receptor ◽  
Partial Agonist ◽  
Agonist Activity ◽  
Partial Agonist 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

Discovery of a cholecystokinin analogue with partial agonist activity

1984 ◽  
Vol 247 (3) ◽  
pp. G261-G264 ◽  
Author(s):  
J. M. Howard ◽  
M. Knight ◽  
R. T. Jensen ◽  
J. D. Gardner
Keyword(s):  
Guinea Pig ◽  
Partial Agonist ◽  
Effective Concentration ◽  
Amylase Secretion ◽  
Agonist Activity ◽  
Pancreatic Acini ◽  
Rat Pancreas ◽  
Partial Agonist Activity ◽  
Stimulation Of

In dispersed acini from guinea pig pancreas, cholecystokinin-(27-32)-amide [CCK-(27-32)-NH2] did not stimulate amylase secretion and inhibited the stimulation caused by CCK-(26-33). In dispersed acini from mouse or rat pancreas, CCK-(27-32)-NH2 stimulated amylase secretion. The stimulation of amylase secretion caused by a maximally effective concentration of CCK-(27-32)-NH2 was less than that caused by a maximally effective concentration of cholecystokinin-(26-33), and in contrast to the action of cholecystokinin-(26-33) supramaximal concentrations of CCK-(27-32)-NH2 did not cause submaximal stimulation of amylase secretion. Dibutyryl cGMP and proglumide each inhibited the stimulation of amylase secretion caused by CCK-(27-32)-NH2. CCK-(27-32)-NH2 inhibited binding of 125I-labeled CCK to mouse and rat pancreatic acini. These results indicate that, in mouse and rat pancreatic acini, CCK-(27-32)-NH2 is a partial agonist and that this partial agonist activity is produced by occupation of the CCK receptor by CCK-(27-32)-NH2.

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
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