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Spiperone hydrochloride (Spiroperidol hydrochloride) is a selective dopamine D2 receptor (Ki values of 0.06 nM, 0.6 nM, 0.08 nM, ~350 nM, ~3500 nM for D2, D3, D4, D1 and D5 receptors, respectively) and 5-HT2A/5-HT1A receptor (Kis of 1 nM/49 nM) antagonist. Spiperone hydrochloride is also a selective α1B-adrenoceptor antagonist. Spiperone hydrochloride activates calcium-activated chloride channel (CaCC). Antipsychotic and anti-inflammatory activities[1][2][3][4][5]. | [in vivo]
Spiperone (1.5 mg/kg; intraperitoneal injection; on days 1, 3, 6, 7, and 13-21; C57Bl/6 mice) treatment reduces infiltration of the alveolar interstitium and alveolar ducts with inflammatory cells and prevents the growth of the connective tissue in the parenchyma of Bleomycin lungs[6]. | Animal Model: | C57Bl/6 mice (7-8-week-old) induced pulmonary fibrosis by Bleomycin[6] | | Dosage: | 1.5 mg/kg | | Administration: | Intraperitoneal injection; on days 1, 3, 6, 7, and 13-21 | | Result: | Reduced infiltration of the alveolar interstitium and alveolar ducts with inflammatory cells and prevented the growth of the connective tissue in the parenchyma of bleomycin lungs.
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| [IC 50]
D2 Receptor: 0.06 nM (Ki); D3 Receptor; D4 Receptor; 5-HT2A Receptor: 1 nM (Ki); 5-HT1A Receptor: 49 nM (Ki); α1B-adrenoceptor; Calcium-activated chloride channel; D1 Receptor: ~350 nM (Ki); D3 Receptor: 0.6 nM (Ki); D4 Receptor: 0.08 nM (Ki); D5 Receptor: ~3500 nM (Ki) | [storage]
Store at RT | [References]
[1] P Seeman, et al. Dopamine receptor pharmacology. Trends Pharmacol Sci. 1994 Jul;15(7):264-70. DOI:10.1016/0165-6147(94)90323-9
[2] Lihua Liang, et al. Spiperone, identified through compound screening, activates calcium-dependent chloride secretion in the airway. Am J Physiol Cell Physiol. 2009 Jan;296(1):C131-41. DOI:10.1152/ajpcell.00346.2008
[3] Long Tai Zheng, et al. The antipsychotic spiperone attenuates inflammatory response in cultured microglia via the reduction of proinflammatory cytokine expression and nitric oxide production. J Neurochem. 2008 Dec;107(5):1225-35. DOI:10.1111/j.1471-4159.2008.05675.x
[4] Richard A Glennon, et al. Ketanserin and spiperone as templates for novel serotonin 5-HT(2A) antagonists. Curr Top Med Chem. 2002 Jun;2(6):539-58. DOI:10.2174/1568026023393787
[5] Andrea E Errasti, et al. Human umbilical vein vasoconstriction induced by epinephrine acting on alpha1B-adrenoceptor subtype. Am J Obstet Gynecol. 2003 Nov;189(5):1472-80. DOI:10.1067/s0002-9378(03)00646-x
[6] E G Skurikhin, et al. Effect of spiperone on mesenchymal multipotent stromal and hemopoietic stem cells under conditions of pulmonary fibrosis. Bull Exp Biol Med. 2014 May;157(1):132-7. DOI:10.1007/s10517-014-2508-y |
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