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. 2021 Mar 4;13(3):334. doi: 10.3390/pharmaceutics13030334

Table 3.

TRPV1–4 Expression and Function at the blood–brain barrier (BBB).

Studies Species BBB Source Existence Gene/Protein Analysis Functional Stimulation Functional Inhibition
TRPV1
Golech et al. [44] Human Cultured BMECs (Brain microvascular endothelial cells, passage 7–10) isolated from micro vessels/capillaries + RT-PCR (Reverse Transcription-polymerase Chain Reaction), IF (Immunofluorescence) Capsaicin; AM404; endocannabinoids including 2-arachidonoyl-glycerol (2-AG), anandamide (ANA) and methanandamide (m-ANA) (37 °C, 30 s) Capsazepine; Ca2+-free medium
Hu et al. [62] Rat Isolated single venular capillaries (transendothelial electrical resistance (TEER) value 2400 Ω cm2) + - Capsaicin (37 °C, 60 s) Capsazepine
Brown et al. [63] Mouse 1. Isolated mouse brain micro vessels; 2. bEnd.3 cells - RT-PCR - -
Hatano et al. [44] Human Cultured BMECs - RT-PCR, q-PCR - -
Zhang et al. [64] Mouse Isolated BMECs + RNA Sequencing - -
Yang et al. [65] Mouse 1. In situ identification in murine capillaries marked by CD31; 2. bEnd.3 murine BBB cell line + 1. IF; 2. IF, WB (Western blot) - Capsazepine
Luo et al. [66] Human and Rat 1. Human: primary culture of isolated BMECs; 2. Human BBB cell line hCMEC/D3; 3. Rat: isolated capillaries and primary culture of isolated BMECs + q-PCR - Capsazepine
TRPV2
Brown et al. [63] Mouse 1. Isolated mouse brain micro vessels; 2. bEnd.3 cells + RT-PCR Hypoosmotic stress Ruthenium Red; Ca2+-free medium containing EDTA
Hatano et al. [46] Human Cultured BMECs + RT-PCR, qPCR - -
Zhang et al. [64] Mouse Freshly isolated BMECs + RNA Sequencing - -
Luo et al. [45] Human and Rat 1. Human: primary culture of isolated BMECs; 2. Human BBB cell line hCMEC/D3; 3. Rat: isolated capillaries and primary culture of isolated BMECs + q-PCR, IF, WB Cannabidiol (37 °C, 10 min); Heat Tranilast; Ruthenium Red; siRNA targeting TRPV2
TRPV3
Brown et al. [63] Mouse 1. Isolated mouse brain micro vessels; 2. bEnd.3 cells - RT-PCR - -
Hatano et al. [45] Human Cultured BMECs - RT-PCR - -
Zhang et al. [64] Mouse Freshly isolated BMECs - RNA Sequencing - -
Luo et al. [66] Human and Rat 1. Human: primary culture of isolated BMECs; 2. Human BBB cell line hCMEC/D3; 3. Rat: isolated capillaries and primary culture of isolated BMECs - q-PCR - -
TRPV4
Brown et al. [63] Mouse 1. Isolated mouse brain micro vessels; 2. bEnd.3 cells + RT-PCR Hypoosmotic stress; 4αPDD (37 °C) Ruthenium Red; Ca2+-free medium containing EDTA
Sullivan et al. [67] Human Cultured BMECs (passage 3–4) + RT-PCR, IF GSK1016790A; 4αPDD (37 °C, 0.03–0.57 s) HC-067047
Hatano et al. [46] Human Cultured BMECs + RT-PCR, qPCR, IF Hypoosmotic stress; 4αPDD (37 °C) Ruthenium Red; Ca2+-free medium containing EDTA; siRNA targeting TRPV4
Zhang et al. [64] Mouse Freshly isolated BMECs + RNA Sequencing - -
Harraz et al. [61] Mouse Freshly isolated BMECs + - GSK1016790A; 4αPDD; Carbachol (37 °C) HC-067047; Ruthenium Red; TRPV4-KO mice
Luo et al. [66] Human and Rat 1. Human: primary culture of isolated BMECs; 2. Human BBB cell line hCMEC/D3; 3. Rat: isolated capillaries and primary culture of isolated BMECs + q-PCR, IF, WB GSK1016790A(37 °C, <2 min) RN-1734; Ruthenium Red