Table IV. TZD concentrations in plasma... | Rockefeller University Press

Table IV.

TZD concentrations in plasma and in vitro

TZD	In vivo/clinical			Bilayer experiments		Vesicle experiments
	Total plasma concentration	Free plasma concentration^a	Nominal [TZD]^b	[TZD]_a^c	{TZD}_m^c	m_TZD^c	[TZD]_a^c	{TZD}_m^c	m_TZD^c
	µM	nM	µM	nM	moles/cm²		nM	moles/cm²
Troglitazone	2–6.4^d	2–64	1	80	5 × 10⁻¹³	2 × 10⁻³	130	9 × 10⁻¹³	4 × 10⁻³
Rosiglitazone	0.4–1.7^d	4–17	30	18,000	6 × 10⁻¹²	2 × 10⁻²	22,100	8 × 10⁻¹³	3 × 10⁻²
Pioglitazone	1.5–4.4^e	36	10	5,600^f	2 × 10⁻¹²	10⁻²	6,900	3 × 10⁻¹²	10⁻²
Ciglitazone	37–90^g	1,900–2,700	1	5^f	5 × 10⁻¹³	2 × 10⁻³	9	10⁻¹²	4 × 10⁻³

TZD	In vivo/clinical			Bilayer experiments		Vesicle experiments
	Total plasma concentration	Free plasma concentration^a	Nominal [TZD]^b	[TZD]_a^c	{TZD}_m^c	m_TZD^c	[TZD]_a^c	{TZD}_m^c	m_TZD^c
	µM	nM	µM	nM	moles/cm²		nM	moles/cm²
Troglitazone	2–6.4^d	2–64	1	80	5 × 10⁻¹³	2 × 10⁻³	130	9 × 10⁻¹³	4 × 10⁻³
Rosiglitazone	0.4–1.7^d	4–17	30	18,000	6 × 10⁻¹²	2 × 10⁻²	22,100	8 × 10⁻¹³	3 × 10⁻²
Pioglitazone	1.5–4.4^e	36	10	5,600^f	2 × 10⁻¹²	10⁻²	6,900	3 × 10⁻¹²	10⁻²
Ciglitazone	37–90^g	1,900–2,700	1	5^f	5 × 10⁻¹³	2 × 10⁻³	9	10⁻¹²	4 × 10⁻³

Estimated based on protein binding.

[TZD] where gA channel function is altered.

Estimated as described in Eqs. A7–A9.

FDA (five of the links where the information can be accessed).

Xue et al., 2003.

Based on clogP (legend to Fig. 1).

Torii et al., 1984, and Aleo et al., 2005; values for rats.