RTI uses cookies to offer you the best experience online. By clicking “accept” on this website, you opt in and you agree to the use of cookies. If you would like to know more about how RTI uses cookies and how to manage them please view our Privacy Policy here. You can “opt out” or change your mind by visiting: http://optout.aboutads.info/. Click “accept” to agree.
Identification of 2-({[1-(4-Fluorophenyl)-5-(2-methoxyphenyl)-1H-pyrazol-3-yl]carbonyl)}amino)tricyclo[3.3.1.13,7]decane-2-carboxylic Acid (NTRC-844) as a selective antagonist for the rat neurotensin receptor type 2
Thomas, J. B., Vivancos, M., Giddings, A. M., Wiethe, R. W., Warner, K. R., Murza, A., Besserer-Offroy, E., Longpre, J.-M., Runyon, S. P., Decker, A. M., Gilmour, B. P., & Sarret, P. (2016). Identification of 2-({[1-(4-Fluorophenyl)-5-(2-methoxyphenyl)-1H-pyrazol-3-yl]carbonyl)}amino)tricyclo[3.3.1.13,7]decane-2-carboxylic Acid (NTRC-844) as a selective antagonist for the rat neurotensin receptor type 2. ACS Chemical Neuroscience, 7(9), 1225-1231. https://doi.org/10.1021/acschemneuro.6b00097
Neurotensin receptor type 2 (NTS2) compounds display analgesic activity in animal pain models. We have identified the first high-affinity NTS2-selective antagonist (8) that is active in vivo. This study also revealed that the NTS2 FLIPR assay designation for a compound, agonist, partial agonist, and so forth, did not correlate with its in vivo activity as observed in the thermal tail-flick acute model of pain. This suggests that calcium mobilization is not the signaling pathway involved in NTS2-mediated analgesia as assessed by the thermal tail-flick model. Finally, we found a significant bias between rat and human for compound 9 in the NTS2 binding assay.
