. Author manuscript; available in PMC: 2022 Mar 31.

Published in final edited form as: J Med Chem. 2021 Dec 20;65(1):257–270. doi: 10.1021/acs.jmedchem.1c01432

Table 3.

Metabolic stability and BBB permeability of select CB₁ allosteric modulators.

Cmpd	2^c	17	31	34
Rat liver microsome t_1/2 (min)^a	13.4 ± 4.1	13.7 ± 1.3	14.9 ± 3.5	15.5 ± 0.8
Rat liver microsome Clearance (μL/min/mg)^a	113.7 ± 34.4	102.0 ± 11.0	99.3 ± 23.8	90.0 ± 4.6
%Qh^b	72.6	72.2	70.6	69.8
P_app (A-to-B) (x10⁻⁶ cm/s) ^a	2.6 ± 0	N.D.	19.2 ± 0.4	N.D.
P_app (B-to-A) (x10⁻⁶ cm/s) ^a	2.2 ± 0.1	N.D.	21.3 ± 1.1	N.D.
Efflux BA/AB	0.8	N.D.	1.1	N.D.
Rat Plasma Protein Binding	99.9%	N.D.	99.6%	N.D.
Solubility (μM)	< 0.5	N.D.	< 1.0	N.D.

Values are expressed as mean ± SD from two independent experiments.

Percentage of hepatic blood flow.

Part of data have been previous reported.^{32, 35} N.D. Not determined.