scholarly journals Design and pharmacological characterization of VUF14480, a covalent partial agonist that interacts with cysteine 983.36of the human histamine H4receptor

2013 ◽  
Vol 170 (1) ◽  
pp. 89-100 ◽  
Author(s):  
S Nijmeijer ◽  
H Engelhardt ◽  
S Schultes ◽  
A C van de Stolpe ◽  
V Lusink ◽  
...  
Keyword(s):  
Partial Agonist ◽  
Pharmacological Characterization ◽  
Human Histamine

scholarly journals Pharmacological Characterization of Dezocine, a Potent Analgesic Acting as a κ Partial Agonist and μ Partial Agonist

2018 ◽  
Vol 8 (1) ◽  
Author(s):  
Yu-Hua Wang ◽  
Jing-Rui Chai ◽  
Xue-Jun Xu ◽  
Ru-Feng Ye ◽  
Gui-Ying Zan ◽  
...  
Keyword(s):  
Partial Agonist ◽  
Pharmacological Characterization

Cloning, Expression, and Pharmacological Characterization of a Novel Human Histamine Receptor

2001 ◽  
Vol 59 (3) ◽  
pp. 434-441 ◽  
Author(s):  
Yuan Zhu ◽  
David Michalovich ◽  
Hsiao-Ling Wu ◽  
K. B. Tan ◽  
George M. Dytko ◽  
...  
Keyword(s):  
Histamine Receptor ◽  
Pharmacological Characterization ◽  
Human Histamine

Pharmacological characterization of a novel muscarinic partial agonist, YM796, in transfected cells expressing the m1 or m2 muscarinic receptor gene

Life Sciences ◽  
1992 ◽  
Vol 50 (5) ◽  
pp. 355-363 ◽  
Author(s):  
Hongbing Wei ◽  
William R. Roeske ◽  
Josephine Lai ◽  
Fumikazu Wanibuchi ◽  
Kazuyuki Hidaka ◽  
...  
Keyword(s):  
Muscarinic Receptor ◽  
Partial Agonist ◽  
Receptor Gene ◽  
Pharmacological Characterization ◽  
Transfected Cells ◽  
M2 Muscarinic Receptor

scholarly journals Synthesis, Pharmacological and Structural Characterization of Novel Conopressins from Conus miliaris

Marine Drugs ◽  
2020 ◽  
Vol 18 (3) ◽  
pp. 150 ◽  
Author(s):  
Julien Giribaldi ◽  
Lotten Ragnarsson ◽  
Tom Pujante ◽  
Christine Enjalbal ◽  
David Wilson ◽  
...  
Keyword(s):  
Partial Agonist ◽  
Venom Gland ◽  
Membrane Receptors ◽  
Cone Snail ◽  
Critical Position ◽  
Pharmacological Characterization ◽  
Novel Structure ◽  
Drug Lead ◽  
A Charge

Cone snails produce a fast-acting and often paralyzing venom, largely dominated by disulfide-rich conotoxins targeting ion channels. Although disulfide-poor conopeptides are usually minor components of cone snail venoms, their ability to target key membrane receptors such as GPCRs make them highly valuable as drug lead compounds. From the venom gland transcriptome of Conus miliaris, we report here on the discovery and characterization of two conopressins, which are nonapeptide ligands of the vasopressin/oxytocin receptor family. These novel sequence variants show unusual features, including a charge inversion at the critical position 8, with an aspartate instead of a highly conserved lysine or arginine residue. Both the amidated and acid C-terminal analogues were synthesized, followed by pharmacological characterization on human and zebrafish receptors and structural investigation by NMR. Whereas conopressin-M1 showed weak and only partial agonist activity at hV1bR (amidated form only) and ZFV1a1R (both amidated and acid form), both conopressin-M2 analogues acted as full agonists at the ZFV2 receptor with low micromolar affinity. Together with the NMR structures of amidated conopressins-M1, -M2 and -G, this study provides novel structure-activity relationship information that may help in the design of more selective ligands.

In vitro and in vivo pharmacological characterization of PF-01354082, a novel partial agonist selective for the 5-HT4 receptor

2009 ◽  
Vol 609 (1-3) ◽  
pp. 5-12 ◽  
Author(s):  
Tadayoshi Mikami ◽  
Tohru Komada ◽  
Hiromi Sugimoto ◽  
Keiko Suzuki ◽  
Takashi Ohmi ◽  
...  
Keyword(s):  
Partial Agonist ◽  
Pharmacological Characterization
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