The transient receptor potential channel of the vanilloid receptor type, subtype 1 (TRPV1) is a member if the TRPV family of ion channels. TRPV1 is a non-selective cation channel, with high permeability to calcium and acts as an integrator of noxious stimuli including heat, low pH and capsaicin. TRPV1 is also activated by endogenous lipid agonists and sensitized by inflammatory mediators. It plays an important role in pain signaling as demonstrated through the use of TRPV1 knockout mice and selective antagonists. TRPV1 is functionally expressed on the terminals of primary afferent fibers terminating in the superficial layers of the dorsal spinal cord, with activation of the receptor leading to, amongst other things, release of CGRP. In the current study, we have examined the ability of agonists (endogenous & synthetic) of the TRPV1 receptor to evoke CGRP release from homogenate of adult rat spinal cord using a 96-well filter plate assay with results showing a rank order of potency of Resiniferatoxin > Capsaicin > Arvanil > Olvanil > NADA > OLDA > Anandamide. In addition, we have investigated the potency of a variety of TRPV1 antagonists in blocking capsaicin-induced CGRP release (BCTC > Neurogen > A425619 > AMG 49a > AMGEN I > Renovis > JNJ17203212 > Capsazepine > GSK705498 > AMG9810 > SB366791). These antagonists were also profiled for activity against the sensitized TRPV1 receptor.