BMC Pharmacology

Table 1 Binding affinities of olanzapine, compounds 8a, 8b, and 8c for 5HT _2A , D ₂ , and H ₁ receptors

From: Novel olanzapine analogues presenting a reduced H₁ receptor affinity and retained 5HT_2A/D₂ binding affinity ratio

Compound	K i ± SD^a(nM)			pK_iratio 5HT_2A/D₂
Compound	D₂	5HT_2A	H₁	pK_iratio 5HT_2A/D₂
olanzapine	67.72 ± 9.21	4.22 ± 0.77	0.13 ± 0.02	1.17
8c	54.51 ± 12.12	3.70 ± 0.74	1.95 ± 0.33*	1.16
8b	791.08 ± 83.19**	81.20 ± 2.43*	13.63 ± 2.68***	1.16
8a	3939.90 ± 437.35***	787.00 ± 29.81***	33.50 ± 7.39***	1.16

^a Values are the mean ± SD of four to six experiments and represent the concentration giving half maximal inhibition of [³H]-Spiperone (D₂), [³H]-Ketanserine (5HT_2A), and [³H]-Pyrilamine (H₁) binding to rat tissue homogenate. *P < 0.05, **P < 0.01, and ***P < 0.001vs olanzapine values.

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