Pain

A-967079 (1170613-55-4) is a TRPA1 antagonist. Active in rat models.1 Cell permeable References/Citations1) McGaraughty et al. (2010), TRPA1 modulation of spontaneous and mechanically evoked firing of spinal neurons in...

Ambroxol HCl (18683-91-5) is a radical scavenger with anti-inflammatory activity. Blocks the generation of reactive oxygen species by bronchoalveolar lavage cells, inhibits doxorubicin-induced lipid peroxidation (70 mg/kg in...

AP-18 (55224-94-7) is a selective TRPA1 (transient receptor potential A1) channel blocker (IC50 = 3.1 and 4.5 μM at human and mouse TRPA1 respectively). References/Citations1) Petrus et al. (2007) A role of TRPA1 in...

Capsaicin (404-86-4) is a vanilloid agonist known to activate the transient receptor potential channel vanilloid subfamily member 1 (TRPV1)1,2 and to possess analgesic3, anti-inflammatory4 and hypolocomotor effects5. SEVERE...

Gabapentin (60142-96-3) is an approved drug for treatment of various types of neuropathic pain and some forms of epilepsy.  The mechanism of action of gabapentin is not well understood. Despite being a structural mimic...

HC-067047 (883031-03-6) is a potent reversible and selective TRPV4 antagonist. Active at mouse, human and rat TRPV4, IC50 = 17, 48 and 133 nM respectively. Also inhibits the endogenous TRPV4-mediated response to 4α-PDH...

Icilin (36945-98-9) is an agonist of cold-sensitive TRP channels with 2.5-fold greater efficacy and 200-fold greater potency than menthol (EC50 = 0.36 μM for CRM1, rat orthologue of TRPM8).1 Agonist at TRPM8 (EC50 = 0.2...

JZL-184 (1101854-58-3) inhibits MAG lipase (IC50=8 nM) selectively over FAAH. Irreversible. Cell permeable. References/Citations1) Long et al. (2009), Selective blockade of 2-arachidonoylglycerol hydrolysis produces...

Oxaprozin (21256-18-8) is a clinically useful non-steroidal anti-inflammatory drug.1 In addition to typical NSAID COX inhibition, oxaprozin may also exert anti-inflammatory effects via inhibition of the Akt/IKK/NF-κB...

Polygodial (6754-20-7) is a TRPA1 agonist (EC50=400 nM)1. A naturally occurring drimane sesquiterpene dialdehyde found in a variety of plant species including water pepper (Polygonum hydropiper). Polygodial has been used in...