Table 2 IC50 values and type of inhibition for ciproxifan, l-deprenyl, clorgyline, safinamide and moclobemide using kynuramine (KYN) or serotonin (5-HT) and benzylamine (BZA) or phenylethylamine (PEA) as MAO A and MAO B substrates, respectively.

From: Ciproxifan, a histamine H3 receptor antagonist, reversibly inhibits monoamine oxidase A and B

 

IC50 [μM] ± s.e.m (n)

IC50 [μM] ± s.e.m (n)

Inhibition Type

hMAO

rMAO

A

B

A

B

Substrate

KYN

BZA

KYN

5-HT

PEA

 

Ciproxifan

11.4 ± 1.2 (5)

4.3 ± 0.7 (5)

2.1 ± 0.3 (9)

37.5 ± 0.2 (3)

15.4 ± 0.3 (3)

Reversible

Safinamide

n.d.

n.d.

0.049 ± 0.001 (4)

n.d.

n.d.

Reversible20

Moclobemide

568 ± 115 (3)

n.d.

n.d.

n.d.

n.d.

Reversible32

l -Deprenyl

29.6 ± 3.9 (9)

n.d.

0.037 ± 0.004 (5)

n.d.

n.d.

Mixed/Irreversible33

Clorgyline

0.008 ± 0.001 (4)

n.d.

1.3 ± 0.2 (4)

n.d.

n.d.

Mixed/Irreversible33

  1. IC50 values are given as means ± standard errors of means (s.e.m.) of n independent experiments, each performed at least in duplicates.
  2. n.d. = not determined, l -deprenyl IC50 = 0.036 μM33, clorgyline IC50 = 0.0065 μM33, safinamide IC50 = 0.048 μM20, moclobemide IC50 = 361 μM32.