Spiperone hydrochloride - CAS 2022-29-9
Category: Inhibitor
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Molecular Formula:
C23H26FN3O2.HCl
Molecular Weight:
431.94
COA:
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Targets:
5-HT Receptor | Dopamine Receptor
Description:
Spiperone hydrochloride is a 5-HT2A and selective dopamine D2 receptor antagonist (Ki = 0.06, 0.6, 0.08, ~ 350, ~ 3500 nM for D2, D3, D4, D1 and D5 receptors, respectively) used as an antipsychotic. It also acts as an activator of calcium-activated chloride channels (EC50 = 9.3 µM).
Brife Description:
5-HT2A and dopamien D2 receptor antagonist
Purity:
≥98% by HPLC
Related CAS:
749-02-0 (free base)
Synonyms:
8-[4-(4-Fluorophenyl)-4-oxobutyl]-1-phenyl-1,3,8-triazaspiro[4,5]decan-4-one hydrochloride; SR-01000000261
MSDS:
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Application:
antipsychotic
InChIKey:
QUIKMLCZZMOBLH-UHFFFAOYSA-N
InChI:
InChI=1S/C23H26FN3O2.ClH/c24-19-10-8-18(9-11-19)21(28)7-4-14-26-15-12-23(13-16-26)22(29)25-17-27(23)20-5-2-1-3-6-20;/h1-3,5-6,8-11H,4,7,12-17H2,(H,25,29);1H
Canonical SMILES:
C1CN(CCC12C(=O)NCN2C3=CC=CC=C3)CCCC(=O)C4=CC=C(C=C4)F.Cl
1.Effects of dopaminergic agents on carrageenan hyperalgesia in rats.
Gao X;Zhang Y;Wu G Eur J Pharmacol. 2000 Oct 6;406(1):53-8.
The present study explored the role of central dopaminergic transmission in a model of carrageenan-induced inflammatory pain by examining the effects of selective agonists and antagonists of dopamine receptors. The results were as follow: (1) LY171555 (trans-(-)-4aR-4,4a,5,6,7,8,8a,9-Octahydro-5-propyl-1H-pyrazolo[3, 4-g]quinoline hydrochloride), dopamine D(2) receptor agonist, produced anti-hyperalgesia or hypoalgesia in the inflamed hindpaws and non-inflamed hindpaws, respectively; spiperone hydrochloride (8-[4-(4-Fluorophenyl)-4-oxobutyl]-1-phenyl-1,3,8-triazaspiro[4, 5]decan-4-one hydrochloride), dopamine D(2) receptor antagonist, decreased the pain threshold of the non-inflamed hindpaws. (2) (+/-)-SKF38393 hydrochloride ((+/-)-1-Phenyl-2,3,4, 5-tetrahydro-(1H)-3-benzazepine-7,8-diol hydrochloride), dopamine D(1) receptor agonist, produced anti-hyperalgesia or hypoalgesia when administered in a high dose (600 nmol), and decreased the pain threshold of non-inflamed hindpaws when administered in a low dose (150 nmol); R(+)-SCH23390 hydrochloride (R(+)-7-Chloro-8-hydroxy-3-methyl-1-phenyl-2,3,4, 5-tetrahydro-1H-3-benzazepine hydrochloride), dopamine D(1) receptor antagonist, induced anti-hyperalgesia or hypoalgesia, respectively.
2.A crystallographic and molecular modeling study of butyrophenones.
Liang L;Zhu N;White J;Brown C;Klein-Stevens CL J Pharm Sci. 1998 Dec;87(12):1496-501.
The X-ray crystal structures of four butyrophenone analogues have been completed and are reported herein. These include spiperone hydrochloride (I), N-methylspiperone hydrochloride (II), pimozide (III), and fluspirilene (IV). These structures were compared to other structurally similar molecules with similar pharmacological activity. In addition, a molecular modeling study was done in order to determine the low energy conformations of these molecules. It was found that calculations of parameters that describe the molecular conformations showed that all four molecules were structurally similar. Crystallographic data: [see text].
3.Effects of dopaminergic agents on carrageenan hyperalgesia after intrathecal administration to rats.
Gao X;Zhang Y;Wu G Eur J Pharmacol. 2001 Apr 20;418(1-2):73-7.
The present study explored the role of dopaminergic transmission in spinal cord in a model of carrageenan-induced inflammatory pain by examining the effects of selective agonists and antagonists of dopamine receptors. The results were as follows: (1) trans-(-)-4aR-4,4a,5,6,7,8,8a,9-octahydro-5-propyl-1H-pyrazolo[3,4-g] quinoline hydrochloride (LY171555), a dopamine D(2) receptor agonist, produced anti-hyperalgesia (150 and 300 nmol) or hypoalgesia (300 nmol) in the inflamed hindpaws and non-inflamed hindpaws, respectively; spiperone hydrochloride (8-[4-(4-fluorophenyl)-4-oxobutyl]-1-phenyl-1,3,8-triazaspiro[4,5]decan-4-one hydrochloride), a dopamine D(2) receptor antagonist, decreased the pain threshold of non-inflamed hindpaws (300 nmol). (2) (+/-)-SKF38393 hydrochloride ((+/-)-1-phenyl-2,3,4,5-tetrahydro-(1H)-3-benzazepine-7,8-diol hydrochloride), a dopamine D(1) receptor agonist, had no effect on either hindpaw, even at a higher dose (300 nmol); R(+)-7-Chloro-8-hydroxy-3-methyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride (R(+)-SCH23390 hydrochloride), a dopamine D(1) receptor antagonist, induced anti-hyperalgesia in the inflamed hindpaws (300 nmol). The present results suggest that the dopaminergic system in the spinal cord is involved in the central modulation of inflammatory hyperalgesia, and that the different effects are probably induced by different receptors.
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CAS 2022-29-9 Spiperone hydrochloride

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