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EJNMMI Research

Table 1 Affinities (nM) of IV-OH and reference compounds for sigma receptors

From: Development and evaluation of a novel radioiodinated vesamicol analog as a sigma receptor imaging agent

 

Sigma-1 (K i)

Sigma-2 (K i)

(+)-IV-OH

22.8 (6.3)

146.9 (13.1)

(−)-IV-OH

45.5 (9.8)

165.5 (69.2)

(+)-Ves-OH

178.6 (25.2)

97.2 (3.1)

(+)-Vesamicol

19.1 (1.8)

159.3 (43.9)

Haloperidol

6.4 (0.7)

63.0 (7.2)

Pentazocine

10.0 (1.1)

2,417.7 (326.2)

  1. K i values derived from IC50 values according to the equation: K i = IC50/(1 + C/K d), where C is the concentration of the radioligand, and each K d is the dissociation constant of the corresponding radioligand ([3H]pentazocine to sigma-1 (K d = 19.9 nM) and [3H]DTG to sigma-2 (K d = 22.3 nM)). Values are means (SEM) of three or four experiments.
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