My Dad Can Beat Your Dad: Agonists, Antagonists, Partial Agonists, and Inverse Agonists

2017 ◽  
Vol 53 (2) ◽  
pp. 76-79
Author(s):  
Peter C. Kowalski ◽  
Jonathan S. Dowben ◽  
Norman L. Keltner
Keyword(s):  
Inverse Agonists ◽  
Partial Agonists

scholarly journals Lipid Bilayer Simulations of CXCR4 with Inverse Agonists and Weak Partial Agonists

2003 ◽  
Vol 278 (47) ◽  
pp. 47136-47144 ◽  
Author(s):  
John O. Trent ◽  
Zi-xuan Wang ◽  
James L. Murray ◽  
Wenhai Shao ◽  
Hirokazu Tamamura ◽  
...  
Keyword(s):  
Lipid Bilayer ◽  
Inverse Agonists ◽  
Partial Agonists

2-[N-Acylamino(C1−C3)alkyl]indoles as MT1Melatonin Receptor Partial Agonists, Antagonists, and Putative Inverse Agonists

1998 ◽  
Vol 41 (19) ◽  
pp. 3624-3634 ◽  
Author(s):  
Gilberto Spadoni ◽  
Cesarino Balsamini ◽  
Annalida Bedini ◽  
Giuseppe Diamantini ◽  
Barbara Di Giacomo ◽  
...  
Keyword(s):  
Inverse Agonists ◽  
Partial Agonists

The importance of interactions with helix 5 in determining the efficacy of β-adrenoceptor ligands

2013 ◽  
Vol 41 (1) ◽  
pp. 159-165 ◽  
Author(s):  
Tony Warne ◽  
Christopher G. Tate
Keyword(s):  
Transmembrane Helix ◽  
Binding Pocket ◽  
Pharmacological Properties ◽  
Agonist Binding ◽  
Inverse Agonists ◽  
Inactive State ◽  
Partial Agonists ◽  
Activated State

Structures of the inactive state of the thermostabilized β1-adrenoceptor have been determined bound to eight different ligands, including full agonists, partial agonists, inverse agonists and biased agonists. Comparison of the structures shows distinct differences within the binding pocket that correlate with the pharmacological properties of the ligands. These data suggest that full agonists stabilize a structure with a contracted binding pocket and a rotamer change of serine (5.46) compared with when antagonists are bound. Inverse agonists may prevent both of these occurrences, whereas partial agonists stabilize a contraction of the binding pocket but not the rotamer change of serine (5.46). It is likely that subtle changes in the interactions between transmembrane helix 5 (H5) and H3/H4 on agonist binding promote the formation of the activated state.

scholarly journals Spontaneous Human B2 Bradykinin Receptor Activity Determines the Action of Partial Agonists as Agonists or Inverse Agonists

1999 ◽  
Vol 274 (42) ◽  
pp. 29603-29606 ◽  
Author(s):  
Dana B. Fathy ◽  
Tosso Leeb ◽  
Sandra A. Mathis ◽  
L. M. Fredrik Leeb-Lundberg
Keyword(s):  
Receptor Activity ◽  
Inverse Agonists ◽  
Partial Agonists ◽  
Bradykinin Receptor

The Evolution of Histamine H3 Antagonists/Inverse Agonists

2011 ◽  
Vol 11 (6) ◽  
pp. 648-660 ◽  
Author(s):  
Evan P. Lebois ◽  
Carrie K. Jones ◽  
Craig W. Lindsley
Keyword(s):  
Inverse Agonists ◽  
Histamine H3

Novel Approaches in the Treatment of Antipsychotic-Induced Hyperprolactinemia:The Role of Partial Agonists of D2 Dopaminergic Receptors

2010 ◽  
Vol 4 (3) ◽  
pp. 230-240 ◽  
Author(s):  
Domenico De Berardis ◽  
Tiziano Acciavatti ◽  
Daniela Campanella ◽  
Nicola Serroni ◽  
Luigi Olivieri ◽  
...  
Keyword(s):  
Dopaminergic Receptors ◽  
Partial Agonists ◽  
Novel Approaches
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