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. 2015 Jan 20;6(3):329–333. doi: 10.1021/ml500507v

Table 2. 5-HT2C & 5-HT2B Activity, Microsomal Stability and in vitro Permeability Data for Compounds.

graphic file with name ml-2014-00507v_0008.jpg

      5-HT2C
 5-HT2B
        
Cmpd R logD EC50 (nM)a Emaxa,b Ki (nM)a EC50 (nM)a Emaxa,c Kb (nM)a HLM Clint (mL min–1 mg–1) RRCK (×10–6 cm/s) MDCK-MDR1 AB Papp (×10–6 cm/s) MDCK-MDR1 ER (BA/AB)
7 NHMe 0.4 9 99% 3 1484 69%   19 8 2.5 2.8
21a NHEt 0.6 11 79% 3 18 28%   13 7 1.8 2.3
21b NHCH2iPr 1.7 36 95% 12 nt nt   nt nt nt nt
21c NHCH2cPr 1.2 21 100% 0.5 22 51%   27 2 0.8 6.1
21d NHnPr 1.0 nt nt 4 27 38%   11 4 1.5 3.5
21e NHiPr 1.0 nt nt 13 33 32%   nt 12 nt nt
21f NHBn 1.7 158 37% 22     121 35 2 0.6 3.6
21g NMe2 0.6 nt nt 12 30 38%   43 8 2.1 2.2
21h H 0.5 nt nt 35 27 53%   <8 18 3.9 1.5
a

Values are geometric means of up to five experiments. Differences of <2-fold should not be considered significant.

b

Percent activation by maximum asymptote at 10 μM relative to 5-HT.

c

Percent activation by maximum asymptote at 30 μM relative to 5-HT; nt denotes not tested.