TABLE 7

Compounds increasing cAMP levels

Overview of compounds that increase intracellular cAMP levels, including their primary pharmacological action, effects on ABCA1 and ABCG1 expression (arrows: mRNA, protein), and effects on cellular cholesterol efflux. Effects on ABCA1, ABCG1, and cholesterol efflux are presented as follows: (↓) decreased; (= ) no effect; (↑) increased. Italicized symbols indicate changes in ABCA1 and ABCG1 mRNA levels, whereas nonitalicized symbols indicate protein levels.

Compound	Primary Action	ABCA1		ABCG1		Cholesterol Efflux		Reference
6-Benz-cAMP	PKA agonist	↑	THP-1		—	↑	THP-1	Bingham et al., 2010
8-Bromo-cAMP	cAMP analog	=↑	Skin fibroblasts^{^a}		—	↑	THP-1	Haidar et al., 2002; Lin and Bornfeldt, 2002
8-Bromo-cAMP	cAMP analog	↑	PM		—	↑	Skin fibroblasts^{^a}	Haidar et al., 2002; Lin and Bornfeldt, 2002
8-(4-Chlorophenylthio)adenosine-cAMP	cAMP analog	↑	J774.A1		—	=	THP-1	Sakr et al., 1999; Kellner-Weibel et al., 2003
						↑	J774.A1
						↑	L cells
						=	CHO
						=	Fu5AH
						=	Skin fibroblasts^{^a}
						↑	Mouse PM
8-pcPT-2′-O-Me-cAMP	Epac agonist	↑	THP-1		—	↑	THP-1	Bingham et al., 2010
ATL313	A2AR agonist	↑↑	THP-1	↑↑	THP-1		—	Voloshyna et al., 2013
(Bu)₂cAMP	cAMP analog	↑	RAW264.7		—	↑	RAW264.7	Manna et al., 2015
CGS-21680	A2AR agonist	↑↑	THP-1	↑↑	THP-1	↑	THP-1	Bingham et al., 2010; Voloshyna et al., 2013
Cilomast	PDE4 inhibitor	↑	THP-1		—	↑	THP-1	Lin and Bornfeldt, 2002
Cilomast	PDE4 inhibitor	↑	J774.A1		—	↑	J774.A1	Lin and Bornfeldt, 2002
Cilostazol	PDE3 inhibitor	↑↑	THP-1	↑↑	THP-1	↑	THP-1	Nakaya et al., 2010
		↑↑	RAW264.7	↑↑	RAW264.7	↑	RAW264.7
		↑	MDM^{^a}	↑	MDM^{^a}	↑	MDM^{^a}
		↑	PM^{^b}			↑	RCT^{^b}
		=	Liver^{^b}
		=	Small intestine^{^b}
Dibutyrl cyclic AMP	cAMP analog	↑	RAW264	↑	Monocyte-derived macrop^{^a}	↑	RAW264.7	Abe-Dohmae et al., 2000; Gaidarov et al., 2013
Dibutyrl cyclic AMP	cAMP analog	↑	Monocyte-derived macrop^{^a}	↑	Monocyte-derived macrop^{^a}	↑	Monocyte-derived macrop^{^a}	Abe-Dohmae et al., 2000; Gaidarov et al., 2013
Doxazosin	α-A1 adrenergic receptor antagonist	↑↑	THP-1		—	↑	THP-1	Iwamoto et al., 2007; Tsunemi et al., 2014
		↑↑	RAW264.7			↑	RAW264.7
		↑	NCTC clone 1469
		↑	CHO-K1
		↑↑	Liver^{^b}
Forskolin	Adenylyl cyclase activator	↑	Skin fibroblasts^{^a}		—	↑	THP-1	Haidar et al., 2002; Lin and Bornfeldt, 2002
Forskolin	Adenylyl cyclase activator	↑	Skin fibroblasts^{^a}		—	↑	Skin fibroblasts^{^a}	Haidar et al., 2002; Lin and Bornfeldt, 2002
H89	PKA inhibitor		—	↑	CHO-K1 ABCG1(+12)	↑	CHO-K1 ABCG1(+12)	Gelissen et al., 2012
H89	PKA inhibitor		—	=	CHO-K1 ABCG1(−12)	=	CHO-K1 ABCG1(−12)	Gelissen et al., 2012
IBMX	Nonselective PDE inhibitor		—		—	↑	THP-1	Haidar et al., 2002; Lin and Bornfeldt, 2002
IBMX	Nonselective PDE inhibitor		—		—	↑	Skin fibroblasts^{^a}	Haidar et al., 2002; Lin and Bornfeldt, 2002
KT5720	PKA inhibitor		—		—	↑	CHO-K1 ABCG1(+12)	Gelissen et al., 2012
KT5720	PKA inhibitor		—		—	=	CHO-K1 ABCG1(−12)	Gelissen et al., 2012
Methotrexate	Dihydrofolate reductase inhibitor	↑	PBMCs^{^a}		—			Chen et al., 2011a
Rolipram	PDE4-selective inhibitor	↑↑	THP-1		—	↑	THP-1	Lin and Bornfeldt, 2002
Rolipram	PDE4-selective inhibitor	↑	J774.A1		—	↑	J774.A1	Lin and Bornfeldt, 2002

IBMX, 3-isobutyl-1-methylxanthine; macrop, macrophage; MDM, monocyte-derived macrophage; PBMC, peripheral blood mononuclear cell; PM, peritoneal macrophages.
↵^a Human.
↵^b C57BL/6 mice.