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Chemical Compound Review

AC1NSKGE     N-(4-amino-2-methyl-quinolin- 6-yl)-2-[(4...

Synonyms: JTC-801, JTC801, CHEMBL531742, ATL-146e, cc-187, ...
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Disease relevance of N-(4-amino-2-methyl-6-quinolyl)-2-[(4-ethylphenoxy)methyl]benzamide

 

High impact information on N-(4-amino-2-methyl-6-quinolyl)-2-[(4-ethylphenoxy)methyl]benzamide

  • JTC-801 dose-dependently blocked the N/OFQ- and PGE(2)-induced allodynia, but not the PGF(2alpha)-induced one [2].
  • Moreover, the inhibitory effect of N/OFQ was prevented by peptide ([Nphe(1)]N/OFQ(1-13)-NH(2) and UFP-101) and nonpeptide (J-113397 and JTC-801) NOP receptor selective antagonists [3].
  • These results suggest that N/OFQ is involved in the maintenance of neuropathic pain and that the analgesic effect of JTC-801 on neuropathic pain is mediated by inhibition of NO production by neuronal NOS [1].
  • In the present study, we studied the effect of JTC-801 on neuropathic pain induced by L5 spinal nerve transection in mice [1].
  • 5 The time-dependency of JTC-801 action was studied in CHO cells expressing human NOP receptors [4].
 

Chemical compound and disease context of N-(4-amino-2-methyl-6-quinolyl)-2-[(4-ethylphenoxy)methyl]benzamide

  • Concerning hyperalgesia induced by formalin injection into the hindpaw, JTC-801 dose-dependently suppressed the second phase, but not the first phase, of the licking behavior [5].
 

Anatomical context of N-(4-amino-2-methyl-6-quinolyl)-2-[(4-ethylphenoxy)methyl]benzamide

  • JTC-801 inhibited the binding of [(3)H]-nociceptin to human ORL(1) receptors expressed in HeLa cells with a K(i) value of 44.5 nM [6].
  • Although JTC-801 did not inhibit a CCI-induced decrease in BMC and BMD, it inhibited an increase in the number of osteoclasts in the JTC-801 groups [7].
  • Furthermore, systemic JTC-801 reduced Fos-like immunoreactivity in the dorsal horn of the spinal cord (laminae I/II) [5].
 

Gene context of N-(4-amino-2-methyl-6-quinolyl)-2-[(4-ethylphenoxy)methyl]benzamide

  • Indeed, there is tremendous interest in the pharmaceutical industry in the development of nonpeptide ligands such as the potent ORL1 agonist, Ro 64-6198, as anxiolytics and the ORL1 antagonist JTC-801 as novel analgesics [8].
  • However, a 21 min pre-application time was necessary for J-113397 and JTC-801 to prevent N/OFQ inhibition of [(3)H]-NE overflow [4].
  • Pharmacological profiles of a novel opioid receptor-like1 (ORL(1)) receptor antagonist, JTC-801 [6].
  • Allodynia and hyperalgesia evoked by intrathecal administration of Noc/OFQ (50 pg/mouse) were dose dependently blocked by simultaneous administration of JTC-801 with IC(50) values of 32.2 and 363 pg, respectively [9].
 

Analytical, diagnostic and therapeutic context of N-(4-amino-2-methyl-6-quinolyl)-2-[(4-ethylphenoxy)methyl]benzamide

References

  1. Attenuation of neuropathic pain by the nociceptin/orphanin FQ antagonist JTC-801 is mediated by inhibition of nitric oxide production. Mabuchi, T., Matsumura, S., Okuda-Ashitaka, E., Kitano, T., Kojima, H., Nagano, T., Minami, T., Ito, S. Eur. J. Neurosci. (2003) [Pubmed]
  2. The opioid peptide nociceptin/orphanin FQ mediates prostaglandin E2-induced allodynia, tactile pain associated with nerve injury. Okuda-Ashitaka, E., Minami, T., Matsumura, S., Takeshima, H., Reinscheid, R.K., Civelli, O., Ito, S. Eur. J. Neurosci. (2006) [Pubmed]
  3. Pharmacological profile of nociceptin/orphanin FQ receptors regulating 5-hydroxytryptamine release in the mouse neocortex. Mela, F., Marti, M., Ulazzi, L., Vaccari, E., Zucchini, S., Trapella, C., Salvadori, S., Beani, L., Bianchi, C., Morari, M. Eur. J. Neurosci. (2004) [Pubmed]
  4. Pharmacological profiles of presynaptic nociceptin/orphanin FQ receptors modulating 5-hydroxytryptamine and noradrenaline release in the rat neocortex. Marti, M., Stocchi, S., Paganini, F., Mela, F., De Risi, C., Calo', G., Guerrini, R., Barnes, T.A., Lambert, D.G., Beani, L., Bianchi, C., Morari, M. Br. J. Pharmacol. (2003) [Pubmed]
  5. Anti-allodynic and anti-hyperalgesic effects of nociceptin receptor antagonist, JTC-801, in rats after spinal nerve injury and inflammation. Tamai, H., Sawamura, S., Takeda, K., Orii, R., Hanaoka, K. Eur. J. Pharmacol. (2005) [Pubmed]
  6. Pharmacological profiles of a novel opioid receptor-like1 (ORL(1)) receptor antagonist, JTC-801. Yamada, H., Nakamoto, H., Suzuki, Y., Ito, T., Aisaka, K. Br. J. Pharmacol. (2002) [Pubmed]
  7. Effect of JTC-801 (nociceptin antagonist) on neuropathic pain in a rat model. Suyama, H., Kawamoto, M., Gaus, S., Yuge, O. Neurosci. Lett. (2003) [Pubmed]
  8. Peptide and nonpeptide ligands for the nociceptin/orphanin FQ receptor ORL1: research tools and potential therapeutic agents. Zaveri, N. Life Sci. (2003) [Pubmed]
  9. 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. Muratani, T., Minami, T., Enomoto, U., Sakai, M., Okuda-Ashitaka, E., Kiyokane, K., Mori, H., Ito, S. J. Pharmacol. Exp. Ther. (2002) [Pubmed]
 
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