An antagonist of NR2B subunit-containing NDMA receptors (Kd = 4.2 nM); selective for NR1/NR2B-containing NMDA receptors over NR1

(+)-CP 101,606 – 5 mg

Brand:
Cayman
CAS:
134234-12-1
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

CP 101,606 is a noncompetitive antagonist of NDMA receptors containing the NR2B subunit (Kd = 4.2 nM).{39515} CP 101,606 is highly selective for NR1/NR2B-containing NMDA receptors over NR1, NR2A, and NR2B subunits alone and NR1/NR2A receptors in HEK293 cell homogenates. In vivo, CP 101,606 (30 mg/kg, s.c.) inhibits mechanical hyperalgesia following carrageenan challenge in rats.{39516} It also inhibits licking behavior in rats induced by capsaicin (Item No. 92350) and phorbol-12-myristate-13-acetate (PMA; Item No. 10008014; ED50s = 7.5 and 5.7 mg/kg, respectively). CP 101,606 reverses catalepsy in rats induced by haloperidol (Item No. 12014) with an ED50 value of 0.4 mg/kg.{39517} CP 101,606 (1 mg/kg, s.c.) alone or in combination with L-DOPA methyl ester (Item No. 16149) temporarily improves parkinsonian symptoms in an MPTP model of Parkinson’s disease in rhesus monkeys.  

 

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Description

An antagonist of NR2B subunit-containing NDMA receptors (Kd = 4.2 nM); selective for NR1/NR2B-containing NMDA receptors over NR1, NR2A, and NR2B subunits alone and NR1/NR2A receptors in HEK293 cell homogenates; suppresses mechanical hyperalgesia following carrageenan challenge in rats (30 mg/kg, s.c.); inhibits licking behavior in rats induced by capsaicin and PMA (ED50s = 7.5 and 5.7 mg/kg, respectively); reverses haloperidol-induced catalepsy in rats (ED50 = 0.4 mg/kg); temporarily improves parkinsonian symptoms in an MPTP model of Parkinson’s disease in rhesus monkeys

Formal name: 4-hydroxy-αS-(4-hydroxyphenyl)-βS-methyl-4-phenyl-1-piperidineethanol

Synonyms:  CP 98,113

Molecular weight: 327.4

CAS: 134234-12-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Neuroscience|Neurodegenerative Disorders|Parkinson’s Disease||Research Area|Neuroscience|Pain Research

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