5-HT2 affinities

Affinity values of drugs for agonist or antagonist 5-HT2 recognition sites in mammalian brain.

Drug            antagonist Ki (nM)      agonist Ki (nM)

Agonists

(-)DOB          24                      0.39, 0.62
(+/-)DOB        41                      0.79
(+) DOB         146                     2.3, 18
(+/-)DOI                                1.3
TMFPP           161, 251                16
mCPP            199                     22
Quipazine       228                     17, 31
5-OH-DMT        297                     6
5-MeO-T         305                     5
5-MeO-DMT       616                     15
Spiroxatrine    630
Buspirone       794
RU 24969        777, 1000               42, 91
5-HT            928, 3162               7.8, 3.5
DMT             1183                    64
DP-5-CT         5011                    48
Tryptamine      2055                    320
8-OH-DPAT       5350, 10000             >10000
5-CT            19952                   633, 2700
WB 4101         1258, >10000
GR 43175        195526

Antagonists

Spiperone       0.4, 0.5-1.2, 1.6, 2    0.8, 3.8
Ketanserin      0.39-2.1, 1.2, 3.1      1.3, 4.8
Ritanserin      1.48
(+)Butaclamol   2.4                     13, 29
Chlorpromazine  2.8, 3.3-20             7, 70
Cinanserin      2-41, 4.8, 19, 21       3.8, 7.2
Metergoline     0.28-0.8, 1             2.7
Mesulergine     3.98                    4.5
Methiothepin    0.4-1.9, 1.58           6.5
Pitozefin       0.28-6.5, 4.4
d-LSD           2.6-8.2, 2.5            4.8
DHE             2.5
Cyproheptadine  3.16, 3.46
Mianserin       1.4-13, 5, 7.9
Methysergide    0.94-12, 2.5
Clozapine       2-16, 34
Piremperone     1.58
Amitriptyline   4.2-21
Lisuride        5.01
Chlorimipramine 9.8-82
Haloperidol     22-48
Trazodone       24
Imipramine      37-260
LY 53857        37-260
MDL 72832       158
NAN-190         218
BMY 7378        263
Nomifensine     372
(+/-)Propranolol590-758
Yohimbine       660
(+)Propranolol  2490
MDL 73005       3162
(-)Butaclamol                           10000
ICS 205-930                             17000
Prazosin        >10000                  >10000
Cyanopindolol   31622
SDZ(-)21009     10000
(-)Pindolol     29512-39800
(+/-)CYP        29512
(+)CYP          25118
(-)CYP          26302
(+)Pindolol     38018