First in human evaluation of [18F]PK-209, a PET ligand for the ion channel binding site of NMDA receptors

van der Aart, Jasper; Golla, Sandeep S. V.; van der Pluijm, Marieke; Schwarte, Lothar A.; Schuit, Robert C.; Klein, Pieter J.; Metaxas, Athanasios; Windhorst, Albert D.; Boellaard, Ronald; Lammertsma, Adriaan A.; van Berckel, Bart N. M.

doi:10.1186/s13550-018-0424-2

EJNMMI Research

Table 2 Rate constants obtained using a 2T3k_V_B model and three different plasma input functions (IF) for all subjects

From: First in human evaluation of [¹⁸F]PK-209, a PET ligand for the ion channel binding site of NMDA receptors

		Single scan IF						Within-subject IF			Population IF
		Preferred model	K ₁	V _ND	k ₃	K _i	K_i TRTV	Preferred model	K _i	K_i TRTV	Preferred model	K _i	K_i TRTV
S1	Test	2T3k	0.522	9.64	0.0016	0.0148	− 32%	2T3k	0.0118	6%	2T3k	0.0136	4%
S1	Retest	2T3k	0.420	8.02	0.0014	0.0108	− 32%	2T3k	0.0126	6%	2T3k	0.0142	4%
S2	Test	2T4k	0.577	10.12	0.0016	0.0157	− 23%	2T3k	0.0131	-3%	2T3k	0.0113	18%
S2	Retest	2T3k	0.407	5.90	0.0022	0.0125	− 23%	2T3k	0.0127	-3%	2T3k	0.0136	18%
S3	Test	2T3k	0.341	7.33	0.0024	0.0166	− 9%	2T3k	0.0154	5%	2T3k	0.0193	4%
S3	Retest	2T4k	0.347	6.14	0.0026	0.0152	− 9%	2T4k	0.0162	5%	2T4k	0.0201	4%
S4	Test	2T3k	0.473	9.73	0.0025	0.0235	− 45%	2T3k	0.0202	− 17%	2T3k	0.0147	−24%
S4	Retest	2T3k	0.490	9.34	0.0016	0.0148	− 45%	2T3k	0.0170	− 17%	2T3k	0.0115	−24%
S5	Test	2T3k	0.451	8.64	0.0025	0.0208	− 14%	2T3k	0.0200	− 5%	2T3k	0.0170	−9%
S5	Retest	2T3k	0.465	7.29	0.0026	0.0182	− 14%	2T3k	0.0191	− 5%	2T3k	0.0156	−9%
Mean TRTV			13%	21%	20%	24.3% ± 14.5		7.3% ± 5.6			11.9% ± 8.9
Mean test			0.473	9.09	0.0021	0.0183		0.0161			0.0152
Mean retest			0.426	7.34	0.0021	0.0143		0.0155			0.0150
		Preferred model	K ₁	V _ND	k ₃	K _i	% ΔK_i	Preferred model	K _i	% ΔK_i	Preferred model	K _i	% ΔK_i
S6	Baseline	1T2k	0.528	9.78	0.0005	0.0046	182%	1T2k	0.0038	237%	2T4k	0.0071	113%
S6	Ketamine	2T3k	0.605	9.66	0.0014	0.0129	182%	2T3k	0.0128	237%	2T3k	0.0152	113%
S7	Baseline	2T4k	0.394	6.54	0.0029	0.0182	− 35%	2T4k	0.0170	0%	2T4k	0.0150	8%
S7	Ketamine	2T3k	0.487	9.75	0.0012	0.0118	− 35%	2T3k	0.0169	0%	2T4k	0.0162	8%
S8	Baseline	2T3k	0.683	11.72	0.0007	0.0083	1%	2T3k	0.0220	− 9%	2T3k	0.0183	−9%
S8	Ketamine	2T4k	0.559	10.30	0.0008	0.0084	1%	2T3k	0.0201	− 9%	2T3k	0.0167	−9%
S9	Baseline	2T3k	0.368	7.74	0.0026	0.0193	− 36%	2T3k	0.0200	− 41%	2T3k	0.0114	−62%
S9	Ketamine	2T4k	0.328	6.56	0.0020	0.0124	− 36%	2T3k	0.0118	− 41%	2T3k	0.0044	−62%
S10	Baseline	2T3k	0.488	10.51	0.0014	0.0143	30%	2T3k	0.0105	83%	1T2k	0.0011	−10%
S10	Ketamine	2T3k	0.600	9.84	0.0020	0.0186	30%	2T3k	0.0192	83%	1T2k	0.0010	−10%
Mean baseline			0.492	9.25	0.0016	0.0129			0.0147			0.0106
Mean ketamine			0.516	9.22	0.0015	0.0128			0.0162			0.0107
% Change			5%	0%	−9%	−1%			10%			1%

The unit of K₁ is mL · cm³ · min⁻¹ and the unit of k₃ and K_i is min⁻¹. V_ND equals K₁/k₂
TRTV test–retest variability, %ΔK_i the percentage change from the baseline scan

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