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Table 2 Orexin 2 receptor binding kinetic parameters for DORAs

From: The duration of sleep promoting efficacy by dual orexin receptor antagonists is dependent upon receptor occupancy threshold

Compound

Kd(nM)

T1/2ON (min)

KON(mol-1 · min-1)

T1/2OFF (min)

KOFF(min-1)

Almorexant

0.048

162a

1.58 × 107

268

2.696 × 10-3

Suvorexant

0.401

80.1

7.63 × 106

89.4

7.784 × 10-3

DORA-12

0.157

57.5

2.77 × 107

232

3.154 × 10-3

MK-6096

0.338

62.9

1.69 × 107

118

6.754 × 10-3

DORA-22

0.834

24.7

9.19 × 106

37.8

1.878 × 10-2

SB-649868

0.163

37.0

2.56 × 107

57.0

1.258 × 10-2

  1. aAlmorexant T1/2 ON represents an underestimate as almorexant was applied at concentrations 3-fold above its Kd in order to measure its kinetics alongside other DORAs.
  2. Kd, binding constant; KOFF, dissociation constant; KON, association constant; T1/2 OFF, half-life off-rates; T1/2 ON, binding half-life.
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BMC Neuroscience

ISSN: 1471-2202

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