Table 1 EC50 and IC50 values of 5-HT receptors ligands determined by Ca2+, cAMP and reporter gene assays in transfected CHO-K1 cells

From: Luciferase Reporter Gene Assay on Human 5-HT Receptor: Which Response Element Should Be Chosen?

 

Reporter Gene Response/CHO-K1

cAMP Response/CHO-K1

Ca2+ Response/CHO-K1

  

EC50/IC50(nM)

EC50/IC50(nM)

EC50(nM)

 

Compounds

CRE

NFAT

SRE

 

-

5-HT1A

5-HT

6.2 ± 1.2

0.8 ± 0.3

15.5 ± 13.7

290.0, (146.013), (14.714)

(7.415)

 

8-OH-DPAT

7.0 ± 2.9

-

-

(73.013), (6.014)

(9.515)

Methiothepin

110.0 ± 43.0b

-

-

(30.014)a

-

WAY100635

575.0 ± 57.0b

-

-

-

-

5-HT2A

5-HT

180.0 ± 17.0

230.0 ± 90.0

120.0 ± 56.0

-

(30.916)

 

DOI

33.2 ± 4.1

-

-

-

(0.916)

Methiothepin

39.8 ± 4.0b, 5.0 ± 3.4c

-

-

-

-

katanserin

63.1 ± 7.8b

-

-

-

-

5-HT7A

5-HT

80.0 ± 11.2

150.0 ± 20.0

13.4 ± 0.3

230.0, (81.217)

-

 

8-OH-DPAT

110.0 ± 5.6

-

-

(4.017)

-

Methiothepin

64.6 ± 23.2a, 110.0 ± 39.0b

-

-

125.0b, (31.718)b

-

SB269970

680.0 ± 110.0b

-

-

(575.017)b

-

  1. The CHO-K1 cells were co-transfected with luciferase plasmid, 5-HT receptor plasmids and pRL-SV40 plasmid. After the cells were incubated with different concentrations of agonists, luciferase activity was measured. EC50 and IC50 values were generated using origin7.5 software. (a: treated with 8-OH-DPAT; b: treated with 5-HT; c: treated with DOI; “–”: Not available. The values in “()” are from references 13,14,15,16,17,18).
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