A 5-HT1A agonist (IC50 = 4.3 nM in a radioligand binding assay); selective for 5-HT1A over 5-HT2 and α1-adrenergic receptors (IC50s = 697 and 630 nM

Xaliproden (hydrochloride) – 5 mg

Brand:
Cayman
CAS:
90494-79-4
Storage:
-20
UN-No:
Non-Hazardous - /

Xaliproden is an agonist of the serotonin (5-HT) receptor subtype 5-HT1A (IC50 = 4.3 nM in a radioligand binding assay).{59032} It is selective for 5-HT1A over 5-HT2 and α1-adrenergic receptors (IC50s = 697 and 630 nM, respectively), as well as a panel of 13 additional neurotransmitter receptors and ion channels (IC50s = ≥10 µM for all) but also binds sigma (σ) receptors (IC50 = 73 nM). Xaliproden (250 nM) increases NGF-induced neurite outgrowth and α-actinin levels in PC12 cells.{59033} It decreases hippocampal neuronal damage and reduces impairments in sensorimotor function in rat models of transient global ischemia induced by four-vessel occlusion (4-VO) and sciatic nerve crush injury, respectively, when administered at a dose of 10 mg/kg per day.{59034} Xaliproden (10 mg/kg per day) inhibits CNS mononuclear cell infiltration and increases in cerebrospinal fluid IgG levels in a rat model of experimental autoimmune encephalomyelitis (EAE) induced by myelin basic protein.{59035}  

 

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Description

A 5-HT1A agonist (IC50 = 4.3 nM in a radioligand binding assay); selective for 5-HT1A over 5-HT2 and α1-adrenergic receptors (IC50s = 697 and 630 nM, respectively), as well as a panel of 13 additional neurotransmitter receptors and ion channels (IC50s = ≥10 µM for all) but also binds σ receptors (IC50 = 73 nM); increases NGF-induced neurite outgrowth and α-actinin levels in PC12 cells at 250 nM; decreases hippocampal neuronal damage and reduces impairments in sensorimotor function in rat models of transient global ischemia induced by 4-VO and sciatic nerve crush injury, respectively, at 10 mg/kg per day; inhibits CNS mononuclear cell infiltration and increases in cerebrospinal fluid IgG levels in a rat model of EAE induced by myelin basic protein at 10 mg/kg per day

Formal name: 1,2,3,6-tetrahydro-1-[2-(2-naphthalenyl)ethyl]-4-[3-(trifluoromethyl)phenyl]-pyridine, monohydrochloride

Synonyms:  SR 57746A

Molecular weight: 417.9

CAS: 90494-79-4

Purity: ≥98%

Formulation: A crystalline solid

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