193359-26-1

Basic information

• Product Name: 1-[2-(4-HYDROXYPHENOXY)ETHYL]-4-[(4-METHYLPHENYL)METHYL]-4-PIPERIDINOL MONOHYDROCHLORIDE
• Synonyms: 1-[2-(4-HYDROXYPHENOXY)ETHYL]-4-[(4-METHYLPHENYL)METHYL]-4-PIPERIDINOL MONOHYDROCHLORIDE;CO 101244 HYDROCHLORIDE;1-[2-(4-Hydroxyphenoxy)ethyl]-4-[(4-methylphenyl)methyl]-4-piperidinolhydrochloride;4-Piperidinol, 1-[2-(4-hydroxyphenoxy)ethyl]-4-[(4-Methylphenyl)Methyl]-;1-(2-(4-hydroxyphenoxy)ethyl)-4-(4-methylbenzyl)piperidin-4-ol
• CAS NO: 193359-26-1
• Molecular Formula: C21H28ClNO3
• Molecular Weight: 377.90492
• Mol File: 193359-26-1.mol

Chemical Properties

• Boiling Point: 527.9°Cat760mmHg
• Flash Point: 273.1°C
• Appearance: /
• Density: g/cm³
• Vapor Pressure: 5.65E-12mmHg at 25°C
• Storage Temp.: Store at +4°C
• CAS DataBase Reference: 1-[2-(4-HYDROXYPHENOXY)ETHYL]-4-[(4-METHYLPHENYL)METHYL]-4-PIPERIDINOL MONOHYDROCHLORIDE(CAS DataBase Reference)
• NIST Chemistry Reference: 1-[2-(4-HYDROXYPHENOXY)ETHYL]-4-[(4-METHYLPHENYL)METHYL]-4-PIPERIDINOL MONOHYDROCHLORIDE(193359-26-1)
• EPA Substance Registry System: 1-[2-(4-HYDROXYPHENOXY)ETHYL]-4-[(4-METHYLPHENYL)METHYL]-4-PIPERIDINOL MONOHYDROCHLORIDE(193359-26-1)

Safety Data

• Hazardous Substances Data: 193359-26-1(Hazardous Substances Data)

Usage

Uses

Co 101244 is a highly selective N-methyl-D-aspartate NR2B subtype antagonist.

Biological Activity

Novel, potent and selective antagonist of NR2B-containing NMDA receptors (IC 50 values are 0.043, > 100 and > 100 μ M for NR1A/2B, NR1A/2A and NR1A/2C subunit combinations respectively). Displays neuroprotective effects in vivo and in vitro .

InChI:InChI=1/C21H27NO3.ClH/c1-17-2-4-18(5-3-17)16-21(24)10-12-22(13-11-21)14-15-25-20-8-6-19(23)7-9-20;/h2-9,23-24H,10-16H2,1H3;1H

Relevant articles and documents

4-substituted piperidine analogs and their use as subtype selective NMDA receptor antagonists

PCT No. PCT/US96/20872 Sec. 371 Date Sep. 16, 1998 Sec. 102(e) Date Sep. 16, 1998 PCT Filed Dec. 20, 1996 PCT Pub. No. WO97/23216 PCT Pub. Date Jul. 3, 1997Novel 4-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using 4-substituted piperidine analogs are selective active antagonists of N-methyl-D-aspartate (NMDA) receptor subtypes for treating conditions such as stroke, cerebral ischemia, central nervous system trauma, hypoglycemia, psychosis, anxiety, migraine headaches, glaucoma, CMV retinitis, aminoglycoside antibiotics-induced hearing loss, convulsions, chronic pain, opioid tolerance or withdrawal, urinary incontinence or neurodegenerative disorders, such as lathyrism, Alzheimer's Disease, Parkinsonism and Huntington's Disease are described.

4-HYDROXY-PIPERODINE DERIVATIVES

The present invention relates to compounds of the formula STR1 wherein x is--O--,--NH--,--CH 2--,--CH=,--CO 2--,--CONH--,--CON(lower alkyl)--,--S--and--SO 2--; R. sup.1-R. sup.4 are, independently from each other hydrogen, halogen, hydroxy, amino, nitro, lower-alkyl-sulfonylamido, 1-or 2-imidazolyl, 1-(1,2,4-triazolyl) or acetamido;R 5, R 6 are, independently from each other hydrogen, lower-alkyl, hydroxy, lower alkoxy or oxo;R. sup.7-R 10 are, independently from each other hydrogen, lower-alkyl, halogen, trifluoromethyl or lower-alkoxy;n is 0 or 1; and to pharmaceutically acceptable acid addition salts thereof. Compounds of the present invention are NMDA(N-methyl-D-aspartate)-receptor subtype selective blockers.