JTC-801 244218-51-7

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Molecular Weight: 447.96 JTC-801 is a selective opioid receptor-like1 (ORL1) receptor antagonist with IC50 of 94 nM, weakly inhibits receptors δ, κ, and μ.

JTC-801 displays about 12.5-, 129-, and 1055-fold selectivity for ORL1 receptor (Ki = 8.2 nM) over μ-, κ-, and δ-opioid receptors, respectively. JTC-801
does not inhibit forskolin-stimulated cyclic AMP accumulation in human
ORL1 receptor-expressing HeLa cells, but it prevents nociceptin-induced
inhibition of cyclic AMP accumulation, indicating that JTC-801 possesses
full antagonistic activity. In rat cerebrocortical
membrane, JTC-801 inhibits ORL1 receptor with IC50 of 472 nM and
μ-receptor with IC50 of 1831 nM. JTC-801 completely antagonizes the
suppression of nociceptin on forskolin-induced accumulation of cyclic
AMP with IC50 of 2.58 μM in HeLa cells expressing ORL1 receptor.

Oral administration of JTC-801 (0.3-3 mg/kg) antagonizes
nociceptin-induced allodynia in mice, and shows analgesic effect in a
hot plate test using mice and in a formalin test using rats. In mouse hot-plate test, JTC-801 prolongs escape response latency (ERL)
or 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/kg71 by i.v. or 1 mg/kg by p.o. JTC-801 dose-dependently normalizes paw withdrawal latency (PWL).


Although JTC-801 does not inhibit a chronic constriction injury
(CCI)-induced decrease in bone mineral content (BMC) and bone mineral
density (BMD), it inhibits an increase in the number of osteoclasts. Tactile allodynia induced by L5/L6 spinal nerve ligation is reversed by
both systemic (3-30 mg/kg) and spinal (22.5 and 45 pg) JTC-801 in a
dose-dependent manner. Furthermore, systemic JTC-801 reduces Fos-like
immunoreactivity in the dorsal horn of the spinal cord (laminae I/II). JTC-801 produces dose-dependent mechanical and cold anti-allodynic
effects with ED50 of 0.83 mg/kg and 1.02 mg/kg, respectively.

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Product Categories : Neuronal Signaling > Opioid Receptor Inhibitor