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Table 4 In vitro and in vivo pharmacological parameters for putative σ1 receptor agonists

From: Candidate 3-benzazepine-1-ol type GluN2B receptor radioligands (11C-NR2B-Me enantiomers) have high binding in cerebellum but not to σ1 receptors

Ligand

Ki for σ1

Refs

Ki for σ2

ED50 in vivo versusa:

 
    

11C-(−)-NR2B-Me

11C-(+)-NR2B-Me

 

(nM)b

 

(nM)c

(nmol/kg)

 

TC1

10

[40]

370

48

64

SA4503

17.4

[41, 42]

1784

43

41

 

4.6

[38, 43]

63

  

(+)-Pentazocine

13.7

[41, 44]

2875

 > 1000

 

( ±)-PPCC

1.5

[45]

50.8

 > 1000

 

PRE-084

44

[46, 47]

 

 > 1000

 

(+)-SKF10047

48

[48]

625

 > 1000

 
  1. aIn rat whole brain
  2. bReference radioligand: 3H-pentazocine
  3. cReference radioligand: 3H-DTG