Naloxone methiodide is a peripherally restricted, non-selective and competitive opioid receptor blocker (antagonist). Naloxone methiodide does not penetrate the BBB (blood-brain barrier).

Physicochemical Properties

Molecular Formula	C20H24INO4
Molecular Weight	469.31
Exact Mass	469.075
CAS #	93302-47-7
PubChem CID	16219719
Appearance	White to off-white solid powder
LogP	2.841
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	5
Rotatable Bond Count	2
Heavy Atom Count	26
Complexity	637
Defined Atom Stereocenter Count	4
SMILES	C[N+]1(CC[C@]23[C@@H]4C(=O)CC[C@]2([C@H]1CC5=C3C(=C(C=C5)O)O4)O)CC=C.[I-]
InChi Key	ICONPJDAXITIPI-UXYWFNEESA-N
InChi Code	InChI=1S/C20H23NO4.HI/c1-3-9-21(2)10-8-19-16-12-4-5-13(22)17(16)25-18(19)14(23)6-7-20(19,24)15(21)11-12;/h3-5,15,18,24H,1,6-11H2,2H3;1H/t15-,18+,19+,20-,21?;/m1./s1
Chemical Name	(4R,4aS,7aR,12bS)-4a,9-dihydroxy-3-methyl-3-prop-2-enyl-2,4,5,6,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-3-ium-7-one;iodide
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vivo	In IL-10−/− mice with colitis, naloxone‐methiodide (10 mg/mL; 200 μL; ip) causes abdominal hypersensitivity[2].
Animal Protocol	Animal/Disease Models: Ten- to twelveweeks old IL-10 gene-deficient male (IL-10−/−) mice on C57BL/6 genetic background[2] Doses: 10 mg/mL; 200 μL Route of Administration: intraperitoneally (ip) Experimental Results: In piroxicam-treated IL-10−/− mice induced abdominal pain.
References	[1]. TRPV1 promotes opioid analgesia during inflammation. Sci Signal. 2019;12(575):eaav0711. Published 2019 Apr 2. [2]. Endogenous control of inflammatory visceral pain by T cell-derived opioids in IL-10-deficient mice. Neurogastroenterol Motil. 2020;32(2):e13743.

Solubility Data

Solubility (In Vitro)

DMSO: 250 mg/mL (532.70 mM) H2O: 25 mg/mL (53.27 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.08 mg/mL (4.43 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.43 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.1308 mL	10.6539 mL	21.3079 mL
	5 mM	0.4262 mL	2.1308 mL	4.2616 mL
	10 mM	0.2131 mL	1.0654 mL	2.1308 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.