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. Author manuscript; available in PMC: 2021 Aug 1.
Published in final edited form as: Chem Biol Drug Des. 2020 Apr 22;96(2):825–835. doi: 10.1111/cbdd.13691

Table 2b.

Affinity of analogs at serotonin receptors

Ki (nM)a
Cmpd # R1 R2 R3 5-HT1Ab 5-HT1Bc 5-HT2Ad 5-HT5Ae 5-HT6e
10 OMe OMe H 110 255 1680 578 5
11 OH OH H 151 451 1564 244 38
12 OMe OMe Me NAf NA 811 286 5
13 OH OH Me 393 1032 352 363 123
8-OH-DPAT 0.81
ergotamine 9.28 6.92
clozapine 3.91 3.88
a.

Experiments conducted in triplicate; SEM values are within 15% of reported values;

b.

[3H]-WAY100635 used as radioligand;

c.

[3H]GR125743 used as radioligand;

d

.[3H]ketanserin used as radioligand;

e.

[3H]LSD used as radioligand;

f.

NA- not active- ligands displayed <10% inhibition in a primary assay at a ligand concentration of 10 μM