Skip to main content

Table 1 Binding affinity constants (pKi) for the α2-adrenergic, dopamine D2-like or serotonin 5-HT1 receptor families and their respective receptor subtypes for dihydroergotamine (DHE), rauwolscine, GR127935 and haloperidol for cloned human receptors (unless otherwise stated)

From: Dihydroergotamine inhibits the vasodepressor sensory CGRPergic outflow by prejunctional activation of α2-adrenoceptors and 5-HT1 receptors

 

pK i values

Receptors Ligands

α2-

D2-like

5-HT1

α 2A

α 2B

α 2C

D2

D3

D4

1Aª

1B

1D

1E

1F

DHE

8.7a

8.0a

9.0a

8.2a

8.2a

8.1a

9.3a

(r)7.8a

8.6a

6.2a

6.9a

Rauwolscine

8.9b

8.9b

9.3b

N.D.

N.D.

6.5c

7.8c

5.5c

N.D.

GR127935

< 6.0 d,*

N.D.

7.2 e

(r)8.8f

8.6g

5.4g

6.4g

Haloperidol

5.8 h,*

9.4i

8.5i

8.8i

N.D.

  1. Data taken from: a[33]; b[34]; c[35]; d[36]; e[37]; f[38]; g[39]; h[40]; i[41]. All data are given as pKi values at human recombinant receptors, except when stated otherwise: rodent (r) receptors; N.D., not determined; *These pK i values are referred for the respective family receptor