The release of excitatory neurotransmitter substance P (SP) is known to trigger pain signals when it binds to neurokinin-1 (NK-1) receptors. Inhibiting the activity of SP can avert spontaneous pain signals to the brain. TY032 is a novel compound created by Victor Hruby and his lab members that is both an opioid agonist and an NK-1 antagonist. TY032 has been demonstrated to provoke analgesic activity through behavioral tests in rodent models while having significantly less unwanted side effects that are observed with an opioid alone such as morphine. Spinal nerve ligation implemented on rats produces tactile allodynia and thermal hypersensitivity. An intrathecal injection of TY032 resulted in a maximal antihypersensitivity. TY032 at doses in the low microgram range resulted in significant pain inhibition when tested with increasing thermal stimuli. In order to test side effects, a 1 μg dosage of TY032 did not impair motor abilities or induce sedation. Naloxone was used to block endogenous opioid and TY032 opioid activity in tail flicking and flinching studies with mice to determine the activity of the NK-1 antagonism of the compound in substance-P induced itching/biting. TY032 was also tested using in vivo microdialysis to determine if it would inhibit morphine-induced dopamine release as well as block morphine-induced place preference. The various behavioral tests indicated that TY032 hinders pain in a dose-dependent mechanism by binding to μ- and δ-opioid receptors and acting as an agonist while also binding to the NK-1 receptors and acting as an antagonist. Preliminary studies in clinical trials with the combination of a NK1 antagonist in the presence of an opioid confirmed these results. These studies demonstrate how novel compounds can be designed and synthesized to target different receptors and to act as both an agonist and antagonist that work together to inhibit pain while reducing unwanted side effects.