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Table 1 Ki values (nM) of reference standards at male and female rat adenosine A1 and A2A receptors

From: On the basis of sex: male vs. female rat adenosine A1/A2A receptor affinity

Reference standard

Ki value ± SEM (nM)a

Selectivity index

Male rA1vs. 0.1 nM [3H]DPCPX

Female rA1vs. 0.1 nM [3H]DPCPX

Male rA2Avs. 4 nM [3H]NECA

Female rA2Avs. 4 nM [3H]NECA

Male rA2AKi/rA1Ki

Female rA2AKi/rA1Ki

CPA

6.5 Â± 0.4a

5 [36]

6 [37, 38]

7 [39]

8 [40]

10 [41, 42]

15 [43]

6.4 Â± 0.7a

858 Â± 155a

163 [39]

331 [43]

400 [38]

557 [36]

852 Â± 175a

132

133

Caffeine

52 800 Â± 7 400a

18 800 [44]

26 000 [45]

41 000 [10]

43 900 [46]

55 000 [47]

38 000 Â± 5 220a

18 637 Â± 4 331a

22 000 [45]

32 500 [44]

43 000 [10]

21 947 Â± 5 143a

0.4

0.6

DPCPX

0.5 Â± 0.1a

0.4 [48]

0.5 [43, 49]

0.5 Â± 0.03a

149 Â± 23a

157 [44]

340 [51]

530 [43]

545 [39]

135 Â± 29a

298

270

Istradefylline

125 Â± 6a

150 [50]

192 [38]

230 [44]

169 Â± 10a

3.3 Â± 0.9a

1 [38]

2 [50, 52]

5 [44]

8 [46]

11 [41]

2.4 Â± 0.4a

0.03

0.01

  1. aInhibition constant (Ki, nM) value is presented as the mean ± standard error of the mean (SEM), radioligand binding assays performed in triplicate. Values without SEM are taken from the literature [10, 36,37,38,39,40,41,42,43,44,45,46,47,48,49,50,51,52]