TABLE 3. Preference of various 5-HT2 antagonists for human 5-HT2 subpopulations.a

5-HT2A

5-HT2B

5-HT2C

 

[Ki (nM) or pA2 value using rat fundus preparation]

Reference:

5-HT2A-preferring

Risperidone

0.4

29

64

(150)

Pirenperone

1.1

61

77

(150)

Spiperone

1.4

590

3,830

(68)

Ketanserin

2.0

395

160

(150)

MDL 11,939

6.1

3,020

1,020

(150)

AMI-193

7.7

710

8,495

(68)

5-HT2B-preferring

LY23728

66

pA2 = 9.17

123

(10)

LY266097

19

pA2 = 9.80

25

(10)

SB 204741

>10,000

79

2,000

(18)

5-HT2B/2C-preferring

SB 206553

1,600

pA2 = 8.48

10

(43)

SB 200646 A

>10,000

630

400

(18)

SDZ SER-082

630

pA2 = 7.34

16

(102)

a Where human 5-HT2B binding data were unavailable in the literature, pA2 values (rat fundus preparation) are given.

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published 2000