JTC 801
JTC 801 Basic information
- Product Name:
- JTC 801
- Synonyms:
-
- JTC 801
- N-(4-Amino-2-methyl-6-quinolinyl)-2-[(4-ethylphenoxy)methyl]benzamidehydrochloride
- N-(4-Amino-2-methyl-6-quinolinyl)-2-[(4-ethylphenoxy)methyl]benzamide monohydrochloride
- JTC 801 HCl
- JTC-801 hydrochloride
- JTC-801/JTC801
- N-(4-AMino-2-Methyl-quinolin-6-yl)-2-(4-ethyl-phenoxyMethyl)-benzaMide hydrochloride
- Benzamide,N-(4-amino-2-methyl-6-quinolinyl)-2-[(4-ethylphenoxy)methyl]-, hydrochloride
- CAS:
- 244218-51-7
- MF:
- C26H25N3O2.ClH
- MW:
- 447.963
- Product Categories:
-
- Inhibitors
- Mol File:
- 244218-51-7.mol
JTC 801 Chemical Properties
- Melting point:
- 235℃
- storage temp.
- Inert atmosphere,2-8°C
- solubility
- DMSO: ≥20mg/mL
- form
- powder
- color
- tan
- InChIKey
- NQLIYKXNAXKMBL-UHFFFAOYSA-N
JTC 801 Usage And Synthesis
Uses
JTC 801 is a novel opioid receptor-like1 (ORL1) receptor antagonist.
Biological Activity
High affinity, selective NOP receptor antagonist (K i = 8.2 nM). Displays approximately 12.5-, 129- and 1055-fold selectivity over human μ -, κ - and δ -opioid receptors respectively. In vivo shows anti-nociceptive effects in acute pain models. Orally active.
in vivo
JTC-801 (≥0.01?mg/kg, i.v. or 1?mg/kg, p.o.) antagonizes the nociceptin-induced allodynia in mice. In mouse hot-plate test, JTC-801 prolongs escape response latency (ERL) to exposed heat stimulus with minimum effective doses (MED) of 0.01?mg/kg by i.v. or 1?mg/kg by p.o. In the rat formalin test, JTC-801 reduces both the first and second phases of the nociceptive response with MED of 0.01?mg/kg by i.v. administration or 1?mg/kg by p.o. administration. This anti-nociceptive action of JTC-801 is not inhibited by naloxone (10?mg/kg, s.c.). JTC-801 antagonizes the ORL1 receptor response, and has efficacious and potent anti-nociceptive effects in acute pain animal models not only by intravenous injection but also oral administration[1]. JTC-801 (0.3 mg/kg) decreases allodynia induced by the intrathecal injection of nociceptin in mice[2]. JTC-801 (6 mg/kg i.p., once daily) reverses SPS-induced mechanical allodynia, thermal hyperalgesia, anxiety-like behaviour and hypocortisolism. JTC-801 treatment also reverses NOP receptor protein and mRNA up-regulation in amygdala and PAG. JTC-801 blocks elevated N/OFQ levels in serum, CSF, PAG and hippocampus at day 21 of SPS[3]. JTC-801 (0.05-5 mg/kg, i.p.) supresses the the analgesic effect of N2O in 129Sv mice by the writhing test and tail flick test[4].
IC 50
NOP Receptor/ORL1
storage
Desiccate at RT
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