TABLE 4

Affinities of S32504 at multiple classes of 5-HT receptor and α-adrenoceptor Data are means ± S.E.M. of two to four determinations, each performed in triplicate. For additional, procedural details, see Millan et al. (2002).


Receptor

Tissue

Radioligand (nM)

S32504

Ropinirole
hD3 CHO cells [125I]Iodosulpride (0.2) 8.05 7.43a
h5-HT1A CHO cells [3H]8-OH-DPAT (0.4) 6.59 ± 0.07 6.54a
h5-HT1B CHO cells [3H]GR125,743 (1.0) <5 <5a
h5-HT1D CHO cells [3H]GR125,743 (1.0) 6.58 ± 0.08 5.86a
h5-HT2A CHO cells [3H]Ketanserin (0.5) 5.28 ± 0.01 <5a
h5-HT2B CHO cells [3H]Mesulergine (1.0) 5.34 ± 0.08 5.42a
h5-HT2C CHO cells [3H]Mesulergine (1.0) <5 <5a
5-HT3 N1E-115 mouse cells [3H]BRL43694 (1.0) <5 <5
5-HT4 Guinea pig striatum [3H]GR113808 (0.1) <5 <5
h5-HT5A CHO cells [3H]LSD (1) <5 <5
h5-HT6 CHO cells [3H]LSD (2) <5 <5
h5-HT7 HEK-293 [3H]LSD (1) 6.18 ± 0.06 5.82 ± 0.10
1 Rat cortex [3H]Prazosin (0.2) <5 <5
1A CHO cells [3H]Prazosin (0.1) <5 <5a
1B CHO cells [3H]Prazosin (0.1) <5 <5a
1D CHO cells [3H]Prazosin (0.1) <5 <5a
2D Rat cortex [3H]RX821,002 (0.4) <5 5.35a
2A CHO cells [3H]RX821,002 (0.7) 5.09 ± 0.05 5.73a
2B CHO cells [3H]RX821,002 (0.4) 5.78 ± 0.14 6.12a
2C
CHO cells
[3H]RX821,002 (0.6)
<5
5.92a
  • h, human; r, rat.

  • a From Millan et al. (2002)