. Author manuscript; available in PMC: 2019 Feb 1.

Published in final edited form as: Biochem Pharmacol. 2018 Jan 9;148:315–328. doi: 10.1016/j.bcp.2018.01.002

Table 5. The effect of D114^3.32E on selected SB269652 derivatives.

Binding affinity and cooperativity values were obtained in competition or interaction binding experiments using the radioligand [³H]spiperone. Values are expressed as mean ± S.D. from four separate experiments.

	WT		D114^3.32E
	pK_B ^a (K_B, μM)	Logα^b (α)	pK_B (K_B, μM) ^a	Logα^b (α)
SB269652	6.11 ± 0.06 (0.78)	−0.54 ± 0.11 (0.28)	6.39 ± 0.06 (0.41)	−0.22 ± 0.09^* (0.60)
MIPS1059	6.56 ± 0.06 (0.28)	-	4.19 ± 0.11^* (64)	-
MIPS1071	5.90 ± 0.07 (1.26)	-	3.89 ± 0.14^* (128)	-
MIPS1868	6.79 ± 0.09 (0.11)	−1.85 ± 0.32 (0.01)	6.16 ± 0.09 ^* (0.69)	−1.39 ± 0.41 (0.04)

Estimate of the negative logarithm of the equilibrium dissociation constant of SB269652,

Logarithm of the affinity cooperativity factor between SB269652 and [³H]spiperone,

P<0.05, significantly different from the corresponding WT receptor parameter, Student’s t-test

Table 5. The effect of D1143.32E on selected SB269652 derivatives.

Table 5. The effect of D114^3.32E on selected SB269652 derivatives.