Shanghai Nianxing Industrial Co., Ltd
China
Product Name: Naltrindolehydrochloride
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Purity: 99.0%
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111469-81-9

111469-81-9 structure

111469-81-9 structure

Name: Naltrindole hydrochloride
Chemical Name: Naltrindole hydrochloride
CAS Number: 111469-81-9
Molecular Formula: C₂₆H₂₇ClN₂O₃
Molecular Weight: 450.95700
Catalog: Signaling Pathways GPCR/G Protein Opioid Receptor
Create Date: 2018-08-14 16:37:17
Modify Date: 2024-01-04 10:40:56
Naltrindole hydrochloride is a highly potent and selective non-peptide δ opioid receptor antagonist with a Ki of 0.02 nM.

Name	Naltrindole hydrochloride
Synonyms	MFCD00069313 NTI NTI hydrochloride Naltrindole (hydrochloride)

Description	Naltrindole hydrochloride is a highly potent and selective non-peptide δ opioid receptor antagonist with a Ki of 0.02 nM.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Opioid Receptor Signaling Pathways >> Neuronal Signaling >> Opioid Receptor Research Areas >> Neurological Disease Research Areas >> Cancer
Target	Ki: 0.02 nM (δ opioid), 64 nM (μ opioid), 66 nM (κ opioid)[1]
In Vitro	Opioid drugs exert a wide spectrum of physiological and behavioral effects. These effects are mediated via membrane-bound receptors, of which the best characterized are the kappa, delta, and mu receptors[1]. Naltrindole inhibits the proliferation of cultured human U266 MM cells in a time- and dose-dependent manner with an EC50 of 16 μM. Treatment of U266 cells with naltrindole significantly decreases the level of the active, phosphorylated form of the kinases, extracellular signal-regulated kinase and Akt, which may be related to its antiproliferative activity[2]. Naltrindole inhibits growth and induces apoptosis in the three characteristic SCLC cell lines, NCI-H69, NCI-H345, and NCI-H510. Naltrindole treatment reduces constitutive phosphorylation of Akt/PKB on serine 473 and threonine 308 in cells and also its downstream effectors glycogen synthase kinase-3β and the Forkhead transcription factors AFX and FKHR[3].
In Vivo	Naltrindole significantly decreases tumor cell volumes in human MM cell xenografts in severe combined immunodeficient mice[2]. In mice, naltrindole at 20 mg/kg s.c. antagonizes the δ-selective agonist effect of [D- Ser, Leu, Thr]enkephalin (DSLET) without blocking the antinociceptive effect of morphine or U50488H. Naltrindole is the only highly selective δ antagonist that is active upon peripheral administration[4]. Acute naltrindole induces significant decreases in external and total ambulation (horizontal activity) and rearing behaviour (vertical activity), as well as a significant increase in grooming frequency. In animals chronically treated with naltrindole there is an increase in total ambulation one day after the discontinuation of the treatment[5].
Cell Assay	U266 cells are plated in 96-well plates at 2000 cells per well in 100 μL of RPMI 1640 medium, supplemented with 10% fetal bovine serum, 100 U/mL penicillin, and 100 μg/mL streptomycin sulfate. Cells are incubated in quadruplicate in the presence of the various antineoplastic agents to construct dose-response curves, alone or in combination with various doses of naltrindole. At the end of the incubation 10 μL of WST-1 cell proliferation reagent is added to each well, and the plates are returned to the incubator for 1 h. Absorbance is then measured[2].
Animal Admin	Rats: Effects of neonatal naltrindole treatments on open field activity is tested in 20-day old rats. The animals are injected chronically with saline or naltrindole (1 mg/kg, s.c.) (from birth to day 19), and 1 day after the discontinuation of this treatment are studied for the acute effects of naltrindole (1 mg/kg, i.p.)[5]. Mice: Naltrindole is dissolved in distilled water to make a 3 mg/mL solution, and mice are injected with 10 mL/kg daily. Human RPMI 8226 multiple myeloma cells are inoculated subcutaneously into both flanks of SCID mice (10 million cells per flank). After 8 days, 12 mice are divided into two groups of six mice each: vehicle-injected and naltrindole-injected (30 mg/kg). Animals are dosed daily for 36 days, and body weights and xenograft tumors are measured twice a week with a digital caliper[2].
References	[1]. Raynor K, et al. Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors. Mol Pharmacol. 1994 Feb;45(2):330-4. [2]. Mundra JJ, et al. Naltrindole inhibits human multiple myeloma cell proliferation in vitro and in a murine xenograft model in vivo. J Pharmacol Exp Ther. 2012 Aug;342(2):273-87. [3]. Chen YL, et al. Inhibition of akt/protein kinase B signaling by naltrindole in small cell lung cancer cells. [4]. Portoghese PS, et al. Naltrindole, a highly selective and potent non-peptide delta opioid receptor antagonist. Eur J Pharmacol. 1988 Jan 27;146(1):185-6. [5]. Fernández B, et al. Postnatal naltrindole treatments induce behavioural modifications in preweanling rats. Neurosci Lett. 2000 Mar 31;283(1):73-6.

Boiling Point	664.2ºC at 760mmHg
Molecular Formula	C₂₆H₂₇ClN₂O₃
Molecular Weight	450.95700
Flash Point	355.5ºC
Exact Mass	450.17100
PSA	68.72000
LogP	4.31250
Vapour Pressure	1.51E-18mmHg at 25°C
Storage condition	2-8℃

Personal Protective Equipment	Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
RIDADR	NONH for all modes of transport
WGK Germany	3

16676-29-2 structure

16676-29-2

59-88-1 structure

59-88-1

~91%

111469-81-9 structure

111469-81-9

Literature: Duval, Romain A.; Lever, John R. Green Chemistry, 2010 , vol. 12, # 2 p. 304 - 309

Precursor 2
16676-29-2 59-88-1
DownStream 0