Table 1. Human kinin B2R binding and pharmacological activities, distribution coefficient and cell permeability values of agents used in the study.

Agents / Code name	Binding hB2R-HEK293T IC50 (nM)	Bioassay hUV IC50 (nM)	Distribution coefficient log D, n-octanol/PBS (pH 7.4)	Cellular incorporation (pmol/106 cells)
				15 min	4 h	24 h
HOE 140	5.3 ± 1.7*	3.8 ± 0.3*	-3.06	0	0	0
FR 173657	37.0 ± 1.6*	6.0 ± 0.8*	2.89	116	139	185
d-Tat-HOE 140 (NG68)	5.2 ± 1.0	18.0 ± 4.0	-3.02	5	14	21
Cholic-HOE 140 (NG134)	19.0 ± 6.5	6.5 ± 2.5	0.21	13	22	63

Values are means ± s.e.m. ^*Data taken from ref. [34]. Binding assays were performed using living adherent HEK-293T cells transiently transfected with hB2R. Pharmacological activities of B2RAs were performed on human de-endothelized umbilical veins (hUV). Distribution coefficient of compounds between n-octanol and 0.1 M sodium phosphate buffer, pH 7.4, was determined by the shake flask methodology. Compound content of the aqueous and octanol phases was quantified by RP-HPLC. Cellular incorporation of B2RAs within MDA-MB-231 cells were assessed using a tandem quadrupole LC-MS/MS system. Results are the average of two independent assays.