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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 2c.

Affinity of analogs at α-adrenergic receptors

Ki (nM)a.
Cmpd # R1 R2 R3 α1Ab α1Bb α2Ac α2Bc α2Cc
10 OMe OMe H 545 2592 1603 1120 774
11 OH OH H 3197 NAd 2590 2197 1106
12 OMe OMe Me 2863 5874 1174 NA 472
13 OH OH Me >10,000 NA NA 5822 1959
prazosin 0.38 0.39
oxymetazoline 9.30 65.58
yohimbine 10.85
a.

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

b.

[3H]Prazosin used as radioligand;

c.

[3H]Rauwolscine used as radioligand;

d.

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