Back One Page
Table 1 Effect of OA agonists on the adenylate-cyclase activity in homogenates of American cockroach nerve cords in study seta
  Compound       pKa  
no. R Vmax (%)
Ka (µM)
 Observed Calculatedb Deviationc
     
AAT
      
1 2-MeO 45.8plus or minus3.2 1506.37 (1218.42-1871.21) 2.82 2.84 -0.02
2 4-Br 45.2plus or minus2.7 93.35 (84.46-103.29) 4.03 4.1 -0.07
3 4-Cl 72.1plus or minus1.2 68.77 (62.72-75.51) 4.16 3.93 0.23
4 4-F 44.0plus or minus0.9 273.39 (252.31-296.76) 3.56 3.69 -0.13
5 4-OH (OA) 100.0plus or minus5.5 6.58 (6.01-7.19) 5.18 5.01 0.17
6 4-Me 52.0plus or minus1.4 77.95 (67.32-90.41) 4.11 4.05 0.06
7 2,4-F2 41.7plus or minus0.2 263.48 (235.45-295.11) 3.58 3.67 -0.09
     
AIT
      
8 Synephrine 57.6plus or minus5.6 150.03 (125.77-179.70) 3.82 3.9 -0.08
9 2-Me,4-Br 41.1plus or minus1.1 23.62 (20.19-27.83) 4.63 4.59 0.04
10 2,4-Me2 55.0plus or minus3.9 13.65 (12.80-14.54) 4.86 4.85 0.01
11 2,6-Et2 50.2plus or minus2.2 26.13 (25.04-27.26) 4.58 4.55 0.03
     
SBAT
      
12 3-F 40.8plus or minus1.5 35.04 (29.43-41.65) 4.46 4.31 0.15
13 3,4-Cl2 52.5plus or minus6.2 17.51 (14.45-21.29) 4.76 4.73 0.03
14 3,5-Cl2 45.7plus or minus4.6 16.25 (13.41-19.80) 4.79 5.15 -0.36
     
AIO
      
15 2,6-Et2 57.9plus or minus1.8 16.84 (13.92-20.19) 4.77 4.83 -0.06
16 2-Et,6-iPr 42.5plus or minus0.8 13.16 (10.39-16.54) 4.88 4.84 0.04
17 CAO 40.0plus or minus1.1 5.07 (4.12-6.14) 5.29 5.15 0.14
     
SPIT
      
18 2,6-Et2 104.0plus or minus1.6 8.08 (6.32-10.26) 5.09 5.16 -0.07
     
AII
      
19 2,6-Me2 47.7plus or minus7.6 15.03 (11.38-19.92) 4.82 4.88 -0.06
20 2-Me,6-Et 47.6plus or minus2.7 9.54 (7.48-12.10) 5.02 5.04 -0.02
21 2,6-Et2 104.6plus or minus1.4 0.76 (0.49-1.13) 6.12 6.12 0
22 2,4,6-Me3 59.1plus or minus10.2 8.40 (5.68-12.34) 5.08 5.06 0.02
aSee the text for experimental details. The adenylate-cyclase activity of P. americana was measured according to Nathanson's procedure and the cAMP levels were measured by a RIA. Basal (control) and OA (100 mM)-stimulated (Vmax) adenylate cyclase activities were 116.2plus or minus5.4 and 1,473.3plus or minus59.3 pmol cAMP/min/mg of protein, respectively. In parentheses, 95% confidence limits are shown. Ka and 95% confidence limit values were calculated with the Macintosh personal computer system using a sigmoidal curve-fitting program designed for log dose-probit activity analyses.
bCalculated by Equation (1).
cIn case predicted activity is overestimated, deviation is obtained by calculating predicted activity subtracted by experimental value and indicated by minus. In case predicted activity is underestimated, deviation is obtained by calculating experimental activity subtracted by predicted value.
Back One Page