. 2021 Nov 3;10(11):2999. doi: 10.3390/cells10112999

Table 1.

mSR-targeting compounds in pre-clinical studies and their correlated effects.

Compound	Receptor	Profile	Cell Line/Model	Pathway	Effect	Ref.
(−)-Epicatechin	ZIP9	agonist	PC3 (PC) MDA-MB-468 (BC)	ERK1/2, JNK and Bax	Proapoptotic action (increased Caspase-3 levels), increased cAMP and intracellular Zn²⁺ levels	[205]
(+)-Catechin	ZIP9	antagonist	PC3 MDA-MB-468	ERK 1/2, JNK and Bax		[205]
Bicalutamide	ZIP9	antagonist	93RS2 (non -cancerous testicular cell line)	ERK1/2, CREB and ATF-1	Reduced claudin-5 and zonula occludens-1 (ZO-1) expression	[206]
Nandrolone	OXER1	antagonist	MCF-7, MDA-MB-231 (BC)	PI3K/Akt/NF-κB and RACK1	Reduced proliferation and migration	[35]
5-oxo-EPE	OXER1	agonist	In vitro assay		Increased β-Arrestin recruitment	[207]
S-230	OXER1	antagonist	In vivo (monkeys), human neutrophils	Gβγ-mediated signaling	Reduced Gβγ-mediated Ca²⁺ mobilization	[208,209]
S-Y048	OXER1	antagonist	In vivo (monkeys), human neutrophils and human eosinophils	Gβγ-mediated signaling	Reduced Gβγ-mediated Ca²⁺ mobilization, actin polymerization and eosinophil infiltration	[210]
S-C025	OXER1	antagonist	In vivo (monkeys), human neutrophils	Gβγ-mediated signaling	Reduced Gβγ-mediated Ca²⁺ mobilization and eosinophil activation	[211]
264	OXER1	antagonist	In vivo (monkeys, rats), monkey eosinophils and monkey neutrophils	Gβγ-mediated signaling	Reduced Gβγ-mediated Ca²⁺ mobilization, actin polymerization and chemotaxis in granulocytes	[212]
DJ-V-159	GPRC6A	agonist	HEK-293 (human embryonic kidney), MIN-6 (mouse pancreatic β-cell) and in vivo (mice)	Gαs-dependent signaling, ERK1/2	Increased cAMP levels, insulin secretion and decreased serum glucose (in vivo, mouse)	[213]
Diltiazem	CaV1.2	antagonist	In vivo (mice)	CaV1.2-PKC	Inhibition of Ca²⁺ influx, PLCδ1	[214]
Lercanidipine	CaV1.2	antagonist	Healthy and pediatric acute myeloid leukemia (AML) mesenchymal stromal cells (MSCs)		Inhibition of Ca²⁺ influx	[215]
Ketamine	CaV1.2	antagonist	In vivo (mice), Xenopus laevis oocytes (ex vivo)		Inhibition of CaV1.2 expression; Ca²⁺ influx; and vascular smooth muscle contraction	[216]
Ritanserin	CaV1.2	antagonist	Rat vascular myocytes (ex vivo)		Inhibition of Ca²⁺ influx; in vitro vasodilation; and vascular smooth muscle relaxation	[217]
(R)-Roscovitine	CaV1.2	antagonist	HEK-293		Slows activation and enhances inactivation	[218]
Metergoline	NaV1.2	antagonist	Xenopus laevis oocytes (ex vivo)		Inhibition of Na⁺ influx	[219]
Ranolazine	NaV1.2	antagonist	CHO		Inhibition of Na⁺ influx	[220]
2,4(5)-diarylimidazoles	NaV1.2	antagonist	In vitro assay		Inhibition of Na⁺ influx	[221]
Org OD 02-0	mPRα	agonist	A549, PC-9 (human lung adenocarcinoma), HBE (human bronchial epithelial) and MCF-7	PKA/CREB and PKA/β-catenin	Inhibition of cell growth and tumor growth (in vivo)	[222]
Ganaxolone	mPRδ	agonist	GT1-7 (rat hypothalamic cells), H19-7 (rat hippocampal neuronal cells)	Gαs-dependent signaling	Reduction of apoptosis and cell death	[223]
AG-205	PGRMC1	antagonist	CHO-K1, HeLa, COS-7, and H4 glioma Cells		Increased endosome formation	[224]
			PaCa-2 cells (pancreatic cancer)	RACK1, alpha-Actinin-1	Reduced PGRMC1 interactions with the actin cytoskeleton	[225]
			Human granulosa/luteal cell	B-cell lymphoma 2 (BCL2) pathway	Increased PGRMC1 monomeric form, increased proapoptotic Harakiri (Hrk) expression	[226]