BMY-14802 hydrochloride

For research use only. Not for therapeutic Use.

  • CAT Number: I004376
  • CAS Number: 105565-55-7
  • Molecular Formula: C18H23ClF2N4O
  • Molecular Weight: 384.85
  • Purity: ≥95%
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BMY-14802 hydrochloride (BMY-14802-1) is a selective and orally active sigma receptor antagonist with an IC50 of 112 nM. BMY-14802 hydrochloride is also a 5-HT1A and adrenergic α1 receptors agonist. BMY-14802 hydrochloride has antipsychotic effects[1][2][3].
Similar to other 5-HT1A agonists, BMY-14802 hydrochloride affects the firing of 5-HTergic and catecholaminergic neurons and affects behaviors mediated by 5-HT in a 5-HT1A-sensitive manner. BMY-14802 hydrochloride is devoid of significant affinity for the D2 receptor[3].
BMY-14802 (5 mg/kg, 10 mg/kg or 20 mg/kg, ip; once) hydrochloride shows anti-dyskinetic efficacy across a 4-fold dose range against L-DOPA-induced dyskinesias (LID) and is also effective in reducing D1 and D2 receptor agonist-induced dyskinesias. Importantly, at anti-LID doses, BMY-14802 hydrochloride does not affect the efficacy of L-DOPA against lesion-induced akinesia[2].


Catalog Number I004376
CAS Number 105565-55-7
Synonyms

1-(4-fluorophenyl)-4-[4-(5-fluoropyrimidin-2-yl)piperazin-1-yl]butan-1-ol;hydrochloride

Molecular Formula C18H23ClF2N4O
Purity ≥95%
InChI InChI=1S/C18H22F2N4O.ClH/c19-15-5-3-14(4-6-15)17(25)2-1-7-23-8-10-24(11-9-23)18-21-12-16(20)13-22-18;/h3-6,12-13,17,25H,1-2,7-11H2;1H
InChIKey NIBVEFRJDFVQLM-UHFFFAOYSA-N
SMILES C1CN(CCN1CCCC(C2=CC=C(C=C2)F)O)C3=NC=C(C=N3)F.Cl
Reference

[1]. J P Yevich, et al. Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents. J Med Chem. 1992 Nov 27;35(24):4516-25.
 [Content Brief]

[2]. Nirmal Bhide, et al. The effects of BMY-14802 against L-DOPA- and dopamine agonist-induced dyskinesia in the hemiparkinsonian rat. Psychopharmacology (Berl). 2013 Jun;227(3):533-44.
 [Content Brief]

[3]. Melanie A Paquette, et al. The sigma-1 antagonist BMY-14802 inhibits L-DOPA-induced abnormal involuntary movements by a WAY-100635-sensitive mechanism. Psychopharmacology (Berl). 2009 Jul;204(4):743-54.
 [Content Brief]

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