RT Journal Article
SR Electronic
T1 Pharmacology of Vanilloid Transient Receptor Potential Cation Channels
JF Molecular Pharmacology
JO Mol Pharmacol
FD American Society for Pharmacology and Experimental Therapeutics
SP 1262
OP 1279
DO 10.1124/mol.109.055624
VO 75
IS 6
A1 Joris Vriens
A1 Giovanni Appendino
A1 Bernd Nilius
YR 2009
UL http://molpharm.aspetjournals.org/content/75/6/1262.abstract
AB Depending on their primary structure, the 28 mammalian transient receptor potential (TRP) cation channels identified so far can be sorted into 6 subfamilies: TRPC (“Canonical”), TRPV (“Vanilloid”), TRPM (“Melastatin”), TRPP (“Polycystin”), TRPML (“Mucolipin”), and TRPA (“Ankyrin”). The TRPV subfamily (vanilloid receptors) comprises channels critically involved in nociception and thermosensing (TRPV1, TRPV2, TRPV3, and TRPV4), whereas TRPV5 and TRPV6 are involved in renal Ca2+ absorption/reabsorption. Apart from TRPV1, the pharmacology of these channels is still insufficiently known. Furthermore, only few small-molecule ligands for non-TRPV1 vanilloid receptors have been identified, and little is known of their endogenous ligands, resulting in a substantial “orphan” state for these channels. In this review, we summarize the pharmacological properties of members of the TRPV subfamily, highlighting the critical issues and challenges facing their “deorphanization” and clinical exploitation. The American Society for Pharmacology and Experimental Therapeutics