TRPV1 Antagonist

SB-366791 is a potent and selective vanilloid receptor (VR1/TRPV1) antagonist (IC₅₀=5.7 nM). SB-366791 can be used for the research of inflammation.

GSK205 is a potent, selective TRPV4 antagonist with an IC₅₀ of 4.19  μM for inhibiting TRPV4-mediated Ca²⁺ influx.

AG1529 is a TRPV1 inhibitor and capsaicinoid-based soft agent with a human TRPV1 IC₅₀ of 0.9-0.93 μM. AG1529 reversibly blocks capsaicin-evoked TRPV1 activation, binds to the TRPV1 capsaicin binding site, moderately affects pH-induced TRPV1 gating, and does not alter voltage- or heat-mediated TRPV1 responses. AG1529 suppresses TRPV1-mediated neuronal excitability, reduces capsaicin- and pH-evoked neuronal firing, abolishes histaminergic and inflammation-mediated TRPV1 sensitization. AG1529 exhibits anti-nociceptive and antipruritic effects, attenuates in vivo hyperalgesia and pruritus, dose-dependently reduces acute histaminergic itch in rodents, and mildly blocks hTRPA1 and hTRPM8 channel activity. AG1529 undergoes hydrolysis and dermal deactivation, minimizes TRPV1-associated side reactions, does not evoke capsaicin-like burning sensation, and does not disrupt physiological thermal regulation. AG1529 can be used for the research of inflammatory cutaneous nociception and acute histaminergic pruritus.

6-Iodonordihydrocapsaicin is a TRPV1 antagonist. 6-Iodonordihydrocapsaicin functionally blocks TRPV1-mediated responses, including capsaicin-induced ion currents in dorsal root ganglion neurons and distension-induced firing of jejunal spinal afferent fibers in mice. 6-Iodonordihydrocapsaicin can be used in the research of visceral pain and anxiety disorders.

JNJ-17203212 is a selective, potent and competitive TRPV1 antagonist. JNJ-17203212 is developed for researching pain management, such as migraine.

Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside is a TRPV1 antagonist and HDAC7 inhibitor. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside blocks TRPV1-mediated calcium influx, suppresses phosphorylation of p65, IκBα, p38, JNK, and ERK1/2, inhibiting NF-κB and MAPK signaling cascades. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside reduces production and gene expression of pro-inflammatory cytokines IL-1β, IL-6, and TNF-α. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside exhibits potent analgesic activity, elevates thermal pain threshold and mechanical pain threshold in murine models. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside restores CD8⁺ T cell infiltration into bladder cancer tumors and improves bladder cancer immunotherapy efficacy. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside can be used for the researches of painand bladder cancer.

TRPV1 antagonist 3 (Compound 7q) is a potent TRPV1 antagonist with an IC₅₀ of 2.66 nM against capsaicin. TRPV1 antagonist 3 is mode-selective, oral bioavailable (F = 60%) and CNS-penetrant.

Dexbrompheniramine ((+)-Brompheniramine; (S)-Brompheniramine) is a dual inhibitor of histamine H1 receptor and TRPV1 receptor that can cross the blood-brain barrier. Dexbrompheniramine exerts its effects by functionally blocking H1 receptor activity and dose-dependently inhibiting TRPV1-mediated calcium responses, including Capsaicin (HY-10448)-induced responses. The combination of Dexbrompheniramine with Cimetidine (HY-14289) eliminates histamine-induced and sham-feeding-induced drinking behavior, whereas Dexbrompheniramine alone does not induce thirst or alter sham-feeding behavior in rats. Dexbrompheniramine can be used in the research of chronic cough and related pathological mechanisms.

Vanilloid receptor antagonist 1 is a potent vanilloid receptor TRPV1 antagonist extracted from patent US8349852B2, compound B8.

L-R4W2 is a potent antagonist of vanilloid receptor 1 (VR1, TRPV1), with an IC₅₀ of 0.1 μM. L-R4W2 may act as a potent analgesic.

TRPV1 antagonist 10 is an orally active and potent TRPV1 antagonist (IC₅₀ = 33.06 nM), moderate to weak URAT1 (IC₅₀ = 22.51 μM) and GLUT9 (60.25% at 50 μM) inhibitor. TRPV1 antagonist 10 has analgesic and urate-lowering effect. TRPV1 antagonist 10 can be studied for research in hyperuricemia and inflammatory pain.

ABT-102 is a potent and highly selective Vanilloid Receptor (TRPV1) receptor antagonist. ABT-102 potently and reversibly increases heat pain thresholds and reduced painfulness of suprathreshold oral/cutaneous heat. ABT-102 reduces nociceptive responses of animals in models of inflammatory, bone cancer, postoperative, and osteoarthritic pain.

V116517 is a potent, orally active transient receptor potential vanilloid (TRPV1) antagonist. V116517 shows potent activity in inhibiting both capsaicin (CAP)- and acid (pH 5)-induced currents in rat DRG neurons expressing native TRPV (IC₅₀=423.2 nM for CAP; IC₅₀=180.3 nM for acid). V116517 can be used for the research of pain.

JTS-653 is a highly potent and selective transient receptor potential vanilloid 1 (TRPV1) antagonist in vitro and in vivo. JTS-653 attenuates chronic pain refractory to non-steroidal anti-inflammatory agents.

L-R4W2 TFA is a potent antagonist of vanilloid receptor 1 (VR1, TRPV1), with an IC₅₀ of 0.1 μM. L-R4W2 TFA may act as a potent analgesic.

MK-2295 (NGD-8243) is a TRPV1 antagonist. MK-2295 is an analgesic agent, and can be used for research of pain.

ABT-116 is an orally active antagonist of transient receptor potential vanilloid type 1 (TRPV1). ABT-116 has analgesic efficacy. ABT-116 can be used for the research of neurological disease.

TRPV1 antagonist 5 (compound 1) is a potent TRPV1 antagonist.

FAAH-IN-10 is a FAAH inhibitor and TRPV1 antagonist, with an IC₅₀ of 0.57 μM against human FAAH. FAAH-IN-10 regulates FAAH activity, antagonizes TRPV1 activity, and exhibits analgesic and anti-inflammatory activities. FAAH-IN-10 does not induce TRPV1-mediated hyperthermia. FAAH-IN-10 can be used for pain-related research.

TRPV1 antagonist 11 (compound 2ac) is a potent TRPV1 antagonist with an IC₅₀ of 29.3 nM. TRPV1 antagonist 11 is a potent μ-opioid receptor (MOR) agonist with a K_i of 60.3 nM. TRPV1 antagonist 11, a pyrimidine piperazine, exhibits pain relieving effects by antagonizing TRPV1 and stimulating MOR. TRPV1 antagonist 11 shows a potent, dose-dependent anti-nociceptive effect in a Formalin-induced pain model in mice.