JTC-801

Last updated
JTC-801
JTC-801.svg
Clinical data
Other namesJTC-801
Identifiers
  • N-(4-amino-2-methylquinolin-6-yl)-2-[(4-ethylphenoxy)methyl]benzamide
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
CompTox Dashboard (EPA)
Chemical and physical data
Formula C26H25N3O2
Molar mass 411.505 g·mol−1
3D model (JSmol)
  • O=C(c1ccccc1COc2ccc(cc2)CC)Nc3ccc4nc(cc(c4c3)N)C
  • InChI=1S/C26H25N3O2/c1-3-18-8-11-21(12-9-18)31-16-19-6-4-5-7-22(19)26(30)29-20-10-13-25-23(15-20)24(27)14-17(2)28-25/h4-15H,3,16H2,1-2H3,(H2,27,28)(H,29,30) X mark.svgN
  • Key:VTGBZWHPJFMTKS-UHFFFAOYSA-N X mark.svgN
 X mark.svgNYes check.svgY  (what is this?)    (verify)

JTC-801 is an opioid analgesic drug used in scientific research. [1] [2]

JTC-801 is a selective antagonist for the nociceptin receptor, also known as the ORL-1 receptor. [3] This was the fourth opioid receptor to be discovered and is still the least understood. The nociceptin receptor has complex effects which are involved in many processes involved in pain and inflammation responses, and activation of this receptor can either increase or reduce pain depending on dose. [4] Drugs acting at the nociceptin receptor may influence the effects of traditional analgesics such as NSAIDs, [5] μ-opioid agonists, [6] and cannabinoids. [7]

JTC-801 is an orally active drug that blocks the nociceptin receptor and produces analgesic effects in a variety of animal studies, and is particularly useful for neuropathic pain and allodynia associated with nerve injury. [8] [9] [10]

See also

References

  1. ↑ Shinkai H, Ito T, Iida T, Kitao Y, Yamada H, Uchida I (November 2000). "4-Aminoquinolines: novel nociceptin antagonists with analgesic activity". Journal of Medicinal Chemistry. 43 (24): 4667–77. doi:10.1021/jm0002073. PMID   11101358.
  2. ↑ Yamada H, Nakamoto H, Suzuki Y, Ito T, Aisaka K (January 2002). "Pharmacological profiles of a novel opioid receptor-like1 (ORL(1)) receptor antagonist, JTC-801". British Journal of Pharmacology. 135 (2): 323–32. doi:10.1038/sj.bjp.0704478. PMC   1573142 . PMID   11815367.
  3. ↑ Sestili I, Borioni A, Mustazza C, Rodomonte A, Turchetto L, Sbraccia M, et al. (December 2004). "A new synthetic approach of N-(4-amino-2-methylquinolin-6-yl)-2-(4-ethylphenoxymethyl)benzamide (JTC-801) and its analogues and their pharmacological evaluation as nociceptin receptor (NOP) antagonists". European Journal of Medicinal Chemistry. 39 (12): 1047–57. doi:10.1016/j.ejmech.2004.09.009. PMID   15571866.
  4. ↑ Muratani T, Minami T, Enomoto U, Sakai M, Okuda-Ashitaka E, Kiyokane K, et al. (October 2002). "Characterization of nociceptin/orphanin FQ-induced pain responses by the novel receptor antagonist N-(4-amino-2-methylquinolin-6-yl)-2-(4-ethylphenoxymethyl) benzamide monohydrochloride". The Journal of Pharmacology and Experimental Therapeutics. 303 (1): 424–30. doi:10.1124/jpet.102.036095. PMID   12235279. S2CID   1162524.
  5. ↑ Okuda-Ashitaka E, Minami T, Matsumura S, Takeshima H, Reinscheid RK, Civelli O, Ito S (February 2006). "The opioid peptide nociceptin/orphanin FQ mediates prostaglandin E2-induced allodynia, tactile pain associated with nerve injury". The European Journal of Neuroscience. 23 (4): 995–1004. doi:10.1111/j.1460-9568.2006.04623.x. PMID   16519664. S2CID   39006891.
  6. ↑ Zaveri N, Jiang F, Olsen C, Polgar W, Toll L (October 2005). "Small-molecule agonists and antagonists of the opioid receptor-like receptor (ORL1, NOP): ligand-based analysis of structural factors influencing intrinsic activity at NOP". The AAPS Journal. 7 (2): E345-52. doi:10.1208/aapsj070234. PMC   2750971 . PMID   16353914.
  7. ↑ Rawls SM, Schroeder JA, Ding Z, Rodriguez T, Zaveri N (August 2007). "NOP receptor antagonist, JTC-801, blocks cannabinoid-evoked hypothermia in rats". Neuropeptides. 41 (4): 239–47. doi:10.1016/j.npep.2007.03.001. PMID   17512052. S2CID   19443938.
  8. ↑ Mabuchi T, Matsumura S, Okuda-Ashitaka E, Kitano T, Kojima H, Nagano T, et al. (April 2003). "Attenuation of neuropathic pain by the nociceptin/orphanin FQ antagonist JTC-801 is mediated by inhibition of nitric oxide production". The European Journal of Neuroscience. 17 (7): 1384–92. doi:10.1046/j.1460-9568.2003.02575.x. PMID   12713641. S2CID   36588304.
  9. ↑ Suyama H, Kawamoto M, Gaus S, Yuge O (November 2003). "Effect of JTC-801 (nociceptin antagonist) on neuropathic pain in a rat model". Neuroscience Letters. 351 (3): 133–6. doi:10.1016/S0304-3940(03)00502-0. PMID   14623124. S2CID   20099481.
  10. ↑ Tamai H, Sawamura S, Takeda K, Orii R, Hanaoka K (March 2005). "Anti-allodynic and anti-hyperalgesic effects of nociceptin receptor antagonist, JTC-801, in rats after spinal nerve injury and inflammation". European Journal of Pharmacology. 510 (3): 223–8. doi:10.1016/j.ejphar.2005.01.033. PMID   15763246.


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