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. Author manuscript; available in PMC: 2016 Aug 8.
Published in final edited form as: Biochem Pharmacol. 2003 Feb 1;65(3):329–338. doi: 10.1016/s0006-2952(02)01488-0

Table 1.

Inhibition of capacitative calcium influx through SOC channels in HL-60 cells by 1,4-dihydropyridines

graphic file with name nihms807288u1.jpg
Compound R1 R2 R3 R4 R5 R6 IC50a (μM) Imaxb (%)
1 H Me COOEt Ph COOMe Me 40 ± 8 75 ± 6
2 H Me COOEt CH=CH–Ph COOMe Me 15 ± 6 50 ± 6
3 H Me COOEt C≡C–Ph COOMe Me NIc NI
4 H Me COOEt 2-Thienyl COOEt Me NI NI
5 H Me COOEt 4-NO2–Ph COOEt Me 6.5 ± 2.8 70 ± 10
6d H Me COOEt 3-NO2–Ph COOMe Me 3.3 ± 1.2 80 ± 6
7 H Me COOEt 3-NO2–Ph COOEt Me 5.0 ± 2.1 90 ± 3
8e H Me COOMe 2-NO2–Ph COOMe Me 16 ± 2 75 ± 3
9 H Me COOEt 3,5-(NO2)2–Ph COOEt Me 7 95
10 H Me COOEt 3-NH2–Ph COOEt Me NI NI
11 H Me COOEt 3-CF3–Ph COOEt Me 2.6 ± 0.6 55 ± 2
12 H Me COOEt 3-(NHCOMe)–Ph COOEt Me NI NI
13 H Me COOEt 4-OMe–Ph COOMe Me 36 ± 3 75 ± 5
14 H Me COOEt 2-CF3–Ph COOMe Me 35 ± 4 75 ± 4
15 H Me COOEt 3-OMe-4-OH–Ph COOMe Me 25 75
16 H Me COOEt 3-NO2–Ph COSEt Me 8 70
17 H Me COOEt 3-NO2–Ph CN Me NI NI
18 H Me COOEt 3-NO2–Ph COO(CH2)2OH Me 30 80
19 H Me COOEt 3-NO2–Ph COO(CH2)2OMe Me >100 NDf
20 H Me COOEt 3-NO2–Ph COOCH2Ph Me 1.8 ± 0.1 95 ± 5
21 H Me COOCH2Ph 3-NO2–Ph COOCH2Ph Me 3.0 ± 1.5 97 ± 2
22 H Me COOEt 3-NO2–Ph COOCH2-(4-NO2)–Ph Me NI NI
23 H Me COOMe 3-NO2–Ph COOMe Me 8.0 ± 4.0 50 ± 5
24 H Et COOEt 3-NO2–Ph COOEt Et 10 55
25 H Me COOEt 3-NO2–Ph COSEt Et 15 75
26 H Me COOEt 3-NO2–Ph COOEt CF3 NI NI
27 H Me COOEt 3-NO2–Ph COOCH2Ph Cyclopropyl NI NI
28 H Me COOEt 3-NO2–Ph COOCH2Ph Cyclobutyl NI NI
29 H Me COOEt Me COOEt Ph NI NI
30 Me Me COOMe 3-NO2–Ph COOMe Me 2.8 ± 0.3 88 ± 4
31 Me Me COOEt 3-NO2–Ph COOEt Me 2.0 ± 0.8 72 ± 11
32 Me Me COOEt 3-NO2–Ph COOMe Me 2.6 ± 1.1 84 ± 12
33 Et Me COOEt 3-NO2–Ph COOMe Me 6 75
34 Allyl Me COOEt 3-NO2–Ph COOMe Me 6.8 ± 1.8 69 ± 7
35 Propargyl Me COOEt 3-NO2–Ph COOMe Me 1.7 ± 1.3 78 ± 12
36 Benzyl Me COOEt 3-NO2–Ph COOMe Me 28 51
a

The IC50 values represent the mean concentration ± SEM (N = 3–6) required for 50% of the maximum inhibition observed for each compound, as shown in Fig. 3A–C. Single values are the average of two determinations.

b

Imax represents the maximum inhibition ± SEM by the DHP of the sustained calcium levels elicited by 10 μM ATP.

c

NI: no inhibition observed at concentrations up to 100 μM.

d

Nitrendipine.

e

Nifedipine.

f

ND=not determined.