Table 3 Transporters and Receptors Affinities for Clomipramine and Citalopram

From: Neonatal Antidepressant Exposure has Lasting Effects on Behavior and Serotonin Circuitry

 

K i (nM)

 

Receptor

Clomipramine (CMI)

Citalopram (CTM)

CMI/CTM a

SERT

0.49

4.82

0.1

DAT

2125

None

0.00001

NET

40.3

8996

0.004

5HT1A

None

None

—

5HT1B

None

None

—

5HT1D

None

Negligible

—

5HT2

n/a

3185

n/a

5HT2A

20.5

5026

0.004

5HT2C

46.2

1562

0.03

5HT3

535

Negligible

0.00001

5HT6

53.8

n/a

n/a

5HT7

127

n/a

n/a

M1

n/a (∼183 based on imipramine)

1430

0.1

α 1

15.5

None

0.00001

α 1a

3.2

None

0.00001

α 2

none

None

—

α 2a

525

None

0.00001

D1

219

n/a

n/a

D2

120

None

0.00001

D3

40

None

0.00001

  1. Ki (inhibition constant) reflects the affinity of the drug for the transporter or receptor, that is, the lower the value the greater the affinity.
  2. a<1 means CMI more potent; >1 means CTM more potent. SERT, serotonin transporter; DAT, dopamine transporter; NET, noradrenaline transporter; none, no affinity; n/a, no data available. Data on drug affinities represent the mean value obtained from NIMH Psychoactive Drug Screening Program (PDSP) database (http://pdsp.cwru.edu/pdsp.asp).
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