BMY 14802 hydrochloride - CAS 105565-55-7
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
5-HT Receptor | Sigma Receptor
BMY 14802 hydrochloride is a potent sigma receptor antagonist (IC50 = 112 nM) with weak affinity for 5-HT1A and α1 receptors. BMY 14802 is potentially used as an atypical antipsychotic agent for schizophrenia treatment.
Brife Description:
sigma receptor antagonist
≥98% by HPLC
Related CAS:
105565-56-8 (free base)
BMS-181100 hydrochloride; BMY 14802 HCl; α-(4-Fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol hydrochloride
potential atypical antipsychotic agent
Canonical SMILES:
1.NPC 16377, a potent and selective sigma-ligand. II. Behavioral and neuroprotective profile.
Clissold DB1, Pontecorvo MJ, Jones BE, Abreu ME, Karbon EW, Erickson RH, Natalie KJ Jr, Borosky S, Hartman T, Mansbach RS, et al. J Pharmacol Exp Ther. 1993 May;265(2):876-86.
6-[6-(4-Hydroxypiperidinyl)hexyloxy]-3-methylflavone HCI, (NPC 16377), a potent and highly selective sigma-site ligand, was evaluated in tests predictive of antipsychotic and neuroprotective potential and for toxicity. Like haloperidol, clozapine and remoxipride, and the sigma-ligands BMY 14802, ifenprodil and rimcazole, NPC 16377 reversed amphetamine-induced hyperactivity and apomorphine-induced climbing in mice. Additional evidence for antipsychotic activity was obtained in rats with NPC 16377, clozapine, BMY 14802, ifenprodil, haloperidol and rimcazole, all of which reduced conditioned avoidance responses at doses that did not reduce escape behavior. NPC 16377 did not induce catalepsy in mice, suggesting a decreased liability for producing extrapyramidal side effects. NPC 16377 extended survival time for mice exposed to a hypoxic environment. In a model of global ischemia using conscious gerbils, NPC 16377 prevented damage to hippocampal CA1 neurons after either intraperitoneal or oral administration.
2.Regulation of [3H]dopamine release from rat striatal slices by sigma receptor ligands.
Gonzalez-Alvear GM1, Werling LL. J Pharmacol Exp Ther. 1994 Oct;271(1):212-9.
Sigma receptors have been located in several areas of the brain that control motor function, including on the dopaminergic projections from substantia nigra to striatum. In the current study, the regulation of N-methyl-D-aspartate-stimulated [3H]dopamine release from slices of rat striatum by several sigma ligands has been tested. Both isomers of the benzomorphans SKF10,047 and pentazocine inhibited the stimulated release of dopamine in a concentration-related manner. All these compounds probably activate sigma and non-sigma receptors, including phencyclidine receptors, over the broad concentration ranges tested. However, concentrations of (+)pentazocine below about 100 nM appear to act solely through sigma receptors. This phase of inhibition was reversed by the sigma antagonist N-[-2-(3,4-dichlorophenyl)ethyl]-N-methyl-2-[1- pyrimidinyl-1-piperazine butanol and by the sigma1-selective antagonist (1-(cyclopropylmethyl)-4-2'4"-fluorophenyl)-(2'-oxoethyl)piperi din e HBr.
3.Intrathecal treatment with sigma1 receptor antagonists reduces formalin-induced phosphorylation of NMDA receptor subunit 1 and the second phase of formalin test in mice.
Kim HW1, Kwon YB, Roh DH, Yoon SY, Han HJ, Kim KW, Beitz AJ, Lee JH. Br J Pharmacol. 2006 Jun;148(4):490-8. Epub 2006 May 8.
Although previous reports have suggested that the sigma 1 (sigma(1)) receptor may be involved in pain sensation, its specific site of action has not been elucidated. The aim of present study was to determine the role of the spinal sigma(1) receptor in formalin-induced pain behavior, spinal cord Fos expression and phosphorylation of N-methyl-D-aspartate receptor subunit 1 (pNR1). Intrathecal (i.t.) pretreatment with the selective sigma(1) receptor antagonist, BD-1047 (N-[2-(3,4-dichlorophenyl)ethyl]-N-methyl-2-(dimethylamino)ethylamine dihydrobromide) (10-100 nmol) dose dependently reduced formalin-induced pain behaviors in second phase, but not first phase, of the formalin test. I.t. injection of BD-1047 also reduced formalin-evoked Fos expression and pNR1 at the protein kinase C-dependent site, serine-896 (Ser896) and the protein kinase A-dependent site, serine-897 (Ser897) in spinal dorsal horn.i.t. BMY-14802 ((alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol hydrochloride) (10-100 nmol, sigma(1) receptor antagonist and 5-HT(1A) receptor agonist) dose dependently reduced formalin-induced pain behaviors in both phases.
4.sigma Receptor antagonists block the development of sensitization to cocaine.
Ujike H1, Kuroda S, Otsuki S. Eur J Pharmacol. 1996 Jan 25;296(2):123-8.
The effects of putative sigma receptor antagonists, BMY-14802 (alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazine), rimcazole and SR-31742A (cis-3-(hexahydroazepin-1-yl)1-(3-chloro-4- cyclohexylphenyl)propene-1), on the development of behavioral sensitization induced by repeated administration of cocaine were investigated. Acute intraperitoneal injection of 15 mg/kg cocaine in rats induced moderate hyperactivity which mainly consisted of sniffing and rearing. These acute effects of cocaine were hardly affected by co-administration of the sigma receptor antagonists, except that BMY-14802 enhanced, but not significantly cocaine-induced locomotion. While repeated cocaine administration induced a progressive increase in stereotyped behaviors and resulted in sensitization, every sigma receptor antagonists tested attenuated the development of sensitization to cocaine. These prophylactic effects of sigma receptor antagonists against cocaine-induced sensitization were confirmed by the challenge test with cocaine alone after an abstinence.
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CAS 105565-55-7 BMY 14802 hydrochloride

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