Table 6.
Antagonism of fluorescent agonist Gi-mediated responses by DPCPX, XAC and CGS15943
Agonist | log KDDPCPX | n | tog KDXAC | n | log KDCGS | n |
---|---|---|---|---|---|---|
NECA | −9.13 ± 0.10 | 7 | −7.86 ± 0.05 | 14 | −8.80 ± 0.10 | 3 |
APrEA-X-BY630 | −8.70 ± 0.09 | 8 | −7.62 ± 0.07 | 7 | −8.58 ± 0.12 | 7 |
ABEA-X-BY630 | −8.69 ± 0.06 | 8 | −7.55 ± 0.08 | 8 | −8.54 ± 0.09 | 8 |
APEA-X-BY630 | −8.61 ± 0.06 | 8 | −7.56 ± 0.08 | 8 | −8.57 ± 0.10 | 8 |
AOEA-X-BY630 | −8.97 ± 0.07 | 3 | −7.87 ± 0.09 | 3 | −8.87 ± 0.15 | 3 |
ADOEA-X-BY630 | −8.67 ± 0.09 | 6 | −7.71 ± 0.07 | 6 | −8.67 ± 0.08 | 6 |
ABEA-dansyl | −8.76 ± 0.06 | 6 | −7.90 ± 0.06 | 6 | −8.78 ± 0.07 | 6 |
ABEA-AO-dansyl | −8.78 ± 0.15 | 5 | −7.74 ± 0.12 | 5 | −8.90 ± 0.19 | 6 |
AUEA-dansyl | −8.80 ± 0.12 | 7 | −7.97 ± 0.10 | 6 | −8.96 ± 0.11 | 7 |
ABEA-X-BYFL | −8.73 ± 0.16 | 5 | −7.83 ± 0.13 | 5 | −8.69 ± 0.15 | 6 |
Values represent mean ± SEM from n separate experiments.
ABEA, N6-(4-aminobutyl)-5′-ethylamino-5′-oxo-5′-deoxyadenosine; ADOEA, N6-(8-amino-3,6-dioxaoctyl)-5′-ethylamino-5′-oxo-5′-deoxyadenosine; AO, 8-aminooctanoyl; AOEA, N6-(8-aminooctyl)-5′-ethylamino-5′-oxo-5′-deoxyadenosine; APEA, N6-(5-aminopentyl)- 5′-ethylamino-5′-oxo-5′-deoxyadenosine; APrEA, N6-(3-aminopropyl)-5′-ethylamino-5′-oxo-5′-deoxyadenosine; AUEA, N6-(11-aminoundecyl)-5′-ethylamino-5′-oxo-5′-deoxyadenosine; CGS 15943, 5-amino-9-chloro-2-(2-furyl)1,2,4-trizolo[1,5-c]quinazoline; DPCPX, 8-cyclopentyl-1,3-dipropylxanthine; NECA, 5′(N-ethylcarboxamido)adenosine; X, 6-aminohexanoyl; XAC, xanthine amine congener.