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. 2014 Mar 24;35(4):602–647. doi: 10.1210/er.2013-1121

Table 2.

Pharmacoperones for GPCRs

GPCR Ligands Refs.
GnRHR Antagonists 376, 424, 432, 546
AVPR2 Both agonists and antagonists 434, 437, 438, 440, 441
Rhodopsin Vitamin A derivatives 446, 449451
MC4R Antagonists and ER-targeted endogenous agonist 94, 374, 452, 454
GCGR Antagonists 368
DP1 Inverse agonist 460
CaSR Allosteric modulators 461465
LHR Allosteric agonist 466
β1-AR Agonists 467
MOR Both agonists and antagonists 468
κ-opioid receptor Both agonists and antagonists 469, 470
DOR Both agonists and antagonists 471
V1a vasopressin receptor Antagonist 472
V1b/V3 vasopressin receptor Antagonist 473
Kinin B1 receptor Antagonist 474
Adenosine A1 receptor Both agonists and antagonists 475
Leukotriene B4 type-2 receptor Both agonist and antagonist 476
D4 DR Both agonist and antagonists 477