Table 1

Comparison of the affinities (Ki values, nM) of various receptor antagonists at dopamine D2 and D4 receptors with their protective effects (at 10-6M) on hippocampal neurons (expressed in % of MTT values vs control group).

D2 subtype Affinity (Ki, nM)

D4 subtype Affinity (Ki, nM)

Neuroprotective activity (% vs control, MTT values)


(+)-butaclamol

0.8

40

464

Clozapine

36–190

1.6–40

340

Chlorpromazine

0.66–1.5

1.15–37

320

Domperidone

0.30

ND

299

Haloperidol

0.35–1

0.84–5.1

271

(±)-sulpiride a

9.2–15

52–1000

199

L-741,742

> 1700

3.5

186

Risperidone

0.3–5.9

0.25–16

162

Haloperidol metabolite

> 10000

ND

108

Raclopride

0.64–1.8

237–620

110

Remoxipride

30–2000

2800–3690

108

U 99194

2281

> 10000

100


Data from [30-32, 39-45]. ND, not determined.

a S-(-)-sulpiride.

Bastianetto et al. BMC Neuroscience 2006 7:28   doi:10.1186/1471-2202-7-28

Open Data