Analog | N1-a | KD1-b | FAAH1-c | S.A.1-d | R.T.1-d | % MPE1-d | % MPE1-e | % MPE1-f |
---|---|---|---|---|---|---|---|---|
O-1625 | 20∶2 | 2.9 ± 0.3 | 55 ± 8 | 14 (5–36) | 13 (6–26) | N.D.1-g | 111 (28–445) | 190 (40–890) |
n-6 | (75) | (70) | (−4.4) | (1) | (73) | (67) | ||
O-1626 | 20∶1 | 17 ± 2.4 | 103 ± 7 | N.D.1-g | 53 (38–75) | N.D.1-g | 68 (17–268) | 75 (28–204) |
n-6 | (70) | (38) | (−2.5) | (2) | (72) | (90) | ||
O-1624 | 20∶0 | 795 ± 72 | 137 ± 22 | 26 (11–64) | N.D.1-g | N.D.1-g | N.D.1-g | N.D.1-g |
(60) | (54) | (−1.3) | (7) | (17) | (15) | |||
O-1623 | 18∶0 | 9.7 ± 1.5 | 48 ± 13 | N.D.1-g | 41 (13–120) | N.D.1-g | N.D.1-g | N.D.1-g |
(58) | (48) | (−3.0) | (10) | (56) | (30) | |||
O-1705 | 16∶0 | N.D. | 78 ± 12 | 18 (11–30) | 10 (8–12) | 15 (9–25) | N.D.1-g | N.D.1-g |
(58) | (60) | (−6.2) | (68) | (45) | (45) | |||
O-1778 | 12∶0 | 2.5 ± 0.3 | 3.0 ± 0.2 | 0.6 (0.2–1.5) | 3.2 (2.6–4.1) | 2.2 (1.5–3.3) | 2.2 (1.5–3.3) | 20 (9–43) |
(75) | (90) | (−6.7) | (100) | (100) | (84) | |||
O-1887 | 8∶0 | >10,000 | 15 ± 3 | 0.6 (0.5–0.7) | 1.0 (0.8–1.2) | 0.5 (0.5–0.6) | 7.7 (2.9–21) | 11 (4.8–27) |
(90) | (−3.8) | (100) | (91) | (93) |
↵1-a Carbon length of the alkyl moiety∶number of unsaturated bonds; n designates position of double bond from terminal carbon.
↵1-b Results (nM) presented as means ± S.E. with maximal displacement provided below in parentheses.
↵1-c Expressed as IC50 values in nanomolar.
↵1-d Spontaneous activity (S.A.), rectal temperature (R.T.), and tail-flick response (% MPE) are expressed as ED50 values (mg/kg) followed by confidence limits in parentheses after i.v. administration. Below the ED50 values are the maximal effects produced.
↵1-e Antinociceptive activity in the tail-flick procedure after i.t. administration. ED50 (CL) expressed as micrograms per mouse with the maximal effect at doses up to 400 μg/mouse in parentheses.
↵1-f Antinociceptive activity in the tail-flick procedure after i.c.v. administration. ED50 (CL) expressed as micrograms per mouse.
↵1-g N.D., could not be determined.