Research Article

Intracellular Loop 2 Peptides of the Human 5HT1a Receptor are Differential Activators of Gi

Table 2

ic2 Peptide mimic effect on [3H]8-OH-DPAT binding. All binding inhibition values are percent of control agonist (ag.) bound. The upper portion of the table is for peptides nearer the C-terminus, including P11 from Thiagaraj et al., 2007 [53]. These peptides decreased the specific high affinity binding of 5HT1aR agonist [3H]-8-OH-DPAT by 50% at the given concentration. The lower portion of the table (P24 on) is the ic2 peptides toward the C terminus. These peptides were less effective at decreasing specific high affinity binding of [3H]-8-OH-DPAT, and values given are percent of control at the given concentration. Values for intracellular cAMP are relative to FSK-stimulated control. All values for incorporation of -[35S]-GTP into Gi are percent of control. Nominal values for control binding were 400 fmoles/mg protein.

PeptideConc. (uM)% cont. ag, bound, (SEM)[cAMP] (SEM)GTP Incorp. (SEM)

Control100 (6)100 (7)
5HT21 (4)168 (12)
P11750 (1)87 (8)100 (3)
P211552 (4)122 (8)158 (11)
P221651 (2)71 (2)128 (9)
P233050 (22)42 (4)188 (10)
P241094 (9)45 (7)146 (17)
P253087 (12)64 (3)126 (10)
P263075 (19)100 (5)111 (9)
P273095 (5)132 (6)130 (7)