TABLE 4.

Effect of ligand‐based activation of NR1I3 (CAR) and NR1I2 (PXR) on expression of ABC transporters and metabolising enzymes in blood–brain barrier endothelial cells

Receptor	Species	Model	Ligand	Effect on expression and/or activity	Reference
NR1I3	Mouse	Isolated capillaries from wild‐type C3H mice	TCPOBOP	↑ P‐gp, Mrp2, Bcrp	(Wang et al., 2010)
		Isolated capillaries from NR1I3 (−/−) C3H mice		N/E
	Rat	Isolated capillaries from Sprague–Dawley rats	Phenobarbital	↑ P‐gp, Mrp2, Bcrp	(Wang et al., 2010)
	Porcine	Primary culture	CITCO	↑ P‐GP, BCRP	(Lemmen, Tozakidis, Bele, & Galla, 2013)
	Human	hCMEC/D3 cells	CITCO	↑ P‐GP	(Chan et al., 2011)
NR1I32	Mouse	Isolated capillaries from wild‐type CB6F1 mice	PCN	↑ P‐gp	(Bauer et al., 2006)
		Isolated capillaries from hNR1I2 humanised CB6F1 mice	Rifampicin Hyperforin	↑ P‐gp
		CD‐1 mice	Dexamethasone	↑ P‐gp (cortical capillaries), N/E Cyp3a11	(Chan et al., 2013)
	Rat	Isolated capillaries from Sprague–Dawley rats	PCN Dexamethasone	↑ P‐gp, Gstp	(Bauer et al., 2004; Bauer et al., 2008)
		Primary culture from Sprague–Dawley rats	Dexamethasone	↑ P‐GP, Mrp2, Bcrp	(Narang et al., 2008)
	Porcine	Primary culture	Rifampicin Hyperforin	↑ P‐GP, BCRP	(Ott et al., 2009); (Lemmen, Tozakidis, & Galla, 2013)
		White large × Landrace hybrid pigs	Rifampicin	N/E CYP3A22 CYP3A29, CYP3A46 and CYP2B22, P‐GP, MRP1, MRP2	(Nannelli et al., 2010)
	Human	hCMEC/D3 cells	Rifampicin SR12813	↑ P‐GP	(Chan et al., 2011)
		Primary culture		↑ CYP3A4, CYP2C9, CYP2E1	(Ghosh et al., 2017)

Note: ↑ denotes increased expression or activity, and ↓ decreased expression or activity.

Abbreviation: N/E, no effect.