93515-00-5

Usage

Uses

2-Iodomelatonin is a potent agonist of the melatonin receptors (MEL-1).

Biological Activity

Potent melatonin agonist (pK i values are 10.55 and 9.87 at human recombinant MT 1 and MT 2 receptors respectively). 2-[ 125 I]-iodomelatonin has been used to identify, characterize and localize melatonin binding sites in the brain and peripheral tissues.

InChI:InChI=1/C13H15IN2O2/c1-8(17)15-6-5-10-11-7-9(18-2)3-4-12(11)16-13(10)14/h3-4,7,16H,5-6H2,1-2H3,(H,15,17)

Upstream product

• 73-31-4 5-methoxy-N-acetyl-tryptamine 

Relevant academic research and scientific papers

Synthesis process of radioactive tracer 2 - iodine melatonin

The invention relates to the technical field of drug synthesis, and provides a synthetic process of a radioactive tracer 2 - iodine melatonin. A mixture of potassium iodide and elementary iodine is selected as an iodide reagent in the reaction process, tetrabutylammonium bromide and cuprous chloride are used as catalysts, and reaction yield and product purity are greatly improved.

Original design of fluorescent ligands by fusing BODIPY and melatonin neurohormone

An original design and synthesis of fluorescent ligands for melatonin receptor studies is presented and consists in the fusion of the endogenous ligand with the fluorescent BODIPY core. Probes I-IV show high affinities for MT1 and MT2 melatonin receptors and exhibit fluorescence properties compatible with cell observation.

A convenient iodination of indoles and derivatives

We report a direct iodination of indole and derivative compounds with iodine monochloride (ICl) in the presence of Celite. This procedure has now been extended to the iodination of substituted indoles, azaindoles and pyrroles. The scope of this procedure

Phenylethynyl and styryl derivatives of imidazole and fused ring heterocycles

This invention relates to a compound and the use of the compound of the formula wherein R1, R2, R3, R4 and R5 are as defined in the description, A signifies —CH═CH— or —C≡C—; and B signifies wherein R

Synthesis of 131I derivatives of indolealkylamines for brain mapping

The synthesis and spectral properties of new radioiodinated indolealkylamines like 2-[131 I]-iodo-N,N-dimethyltryptamine, 2-[131 I]-iodo-N-methyltryptamine, 2-[131 I]-iodo-5-methoxy-N,N-dimethyltryptamine, 2-[131 I]-iodo-5-hydroxy-N,N-dimethyltryptamine (2-[131 I]-iodo-bufotenine), and 2-[131I]-iodo-tryptamine and the known 2-[131I]-iodo-N-acetyl-5-methoxy-tryptamine (2-[131I]-iodo-melatonine) are described herein. These were synthesized by a high-yield novel method, and their spectral properties are fully described. These compounds are of biological importance and can be used for brain mapping with SPECT technology.

Contraceptive and menstrual cycle controlling drug having oncostatic therapeutic properties for treatment of mammary tumors and melanomas, and method therefor

The present invention relates to a drug for human use, having contraceptive and menstrual cycle controlling properties, characterized in that the drug comprises N-acetyl-5-methoxytryptamine or melatonin, in a dose of 100-200 mg per day, N-acetyl-2-bromo-5-methoxytryptamine or 2-bromomelatonin in a dose of 25-50 mg per day, N-acetyl-2-iodo-5-methoxytryptamine or 2-iodomelatonin, in a dose of 20-40 mgs per day, in association with a progestine compound. The administration is carried out for 23 days, by using an association of 2-iodomelatonin and/or melatonin and/or 2-bromomelatonin and a progestinic compound, followed by 5 days in which only 2-iodomelatonin and/or melatonin and/or 2-bromomelatonin is administered; the drug having oncostatic preventive and therapeutic properties, in mammary tumours and melanomas, characterized by the use of 2-iodomelatonin, melatonin and 2-bromomelatonin respectively with doses of 20-40 mgs., 100-200 mgs., 25-50 mg per day; and the drug having moreover antikinetosic properties, and being characterized by the use of 2-iodomelatonin in a dose per day of 2.5 mg.; melatonin, in a dose per day of 10 mg and 2-bromomelatonin in a dose per day of 3.5 mg, either individually and/or in association with the acetyl coenzyme A-(AcCoA), in a dose of 8-10 mg per day.

A method for carrying out the synthesis of a contraceptive and menstrual cycle controlling drug having oncostatic, antikinetosic, preventive and therapeutic properties for treatment of mammary tumours and melanomas.

The present invention relates to a drug for human use, having contraceptive and menstrual cycle controlling properties, characterized in that the said drug comprises N-acetyl-5-methoxytryptamine or melatonin, in a dose of 100-200 mg pro die, N-acetyl-2-bromo-5-methoxytryptamine or 2-bromomelatonin in a dose of 25-50 mg pro die N-acetyl-2-iodo-5-methoxytryptamine or 2-iodomelatonin, in a dose of 20-40 mg pro die, in association with a progestinic compound. The administration is carried out for 23 days, by using an association of 2-iodomelatonin and/or melatonin and/or 2-bromomelatonin and a progestinic compound, followed by 5 days in which only 2-iodomelatonin and/or melatonin and/or 2-bromomelatonin is administered; the drug having oncostatic preventive and therapeutic properties, in mammary tumours and melanomas, characterized by the use of 2-iodomelatonin, melatonin and 2-bromomelatonin respectively with doses of 20-40 mg, 100-200 mg, 25-50 mg pro die; and the said drug having moreover antikinetosic properties, and being characterized by the use of 2-iodomelatonin in a dose pro die of 2.5 mg, melatonin, in a dose pro die of 10 mg and 2-bromomelatonin in a dose pro die of 3.5 mg, either individually and/or in association with the acetyl coenzime A-(AcCoA), in a dose of 8-10 mg pro die.