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Submit ReviewPrazosin hydrochloride is an α1 and α2B-adrenoceptor antagonist. Also a potent antagonist at the melatonin MT3 receptor (Ki = 10.2 nM). In prostate cancer cells, Prazosin induces DNA damage stress, Cdk1 inactivation, G2 checkpoint arrest and apoptosis. In mice bearing prostate cancer xenografts, oral administration of Prazosin reduces tumor mass.
Prazosin hydrochloride is also offered as part of the Tocriscreen FDA-Approved Drugs. 了解 Tocris 化合物库的更多信息。
分子量 | 419.87 |
公式 | C19H21N5O4.HCl |
储存 | Store at RT |
纯度 | ≥99% (HPLC) |
CAS Number | 19237-84-4 |
PubChem ID | 68546 |
InChI Key | WFXFYZULCQKPIP-UHFFFAOYSA-N |
Smiles | Cl.COC1=CC2=NC(=NC(N)=C2C=C1OC)N1CCN(CC1)C(=O)C1=CC=CO1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 25 | ||
ethanol | 5 |
以下数据基于产品分子量 419.87。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.25 mM | 9.53 mL | 47.63 mL | 95.27 mL |
1.25 mM | 1.91 mL | 9.53 mL | 19.05 mL |
2.5 mM | 0.95 mL | 4.76 mL | 9.53 mL |
12.5 mM | 0.19 mL | 0.95 mL | 1.91 mL |
参考文献是支持产品生物活性的出版物。
Mathe et al (1996) Prazosin inhibits MK-801-induced hyperlocomotion and DA release in the nucleus accumbens. Eur.J.Pharmacol. 309 1 PMID: 8864686
Paul et al (1999) Characterisation of 2-[125I]iodomelatonin binding sites in syrian hamster peripheral organs. J.Pharmacol.Exp.Ther. 290 334 PMID: 10381796
Pickering and Niles (1990) Pharmacological characterization of melatonin binding sites in Syrian hamster hypothalamus. Eur.J.Pharmacol. 175 71 PMID: 2157597
Merck Index 12 7897
Lin et al (2007) Prazosin displays anticancer activity against human prostate cancers: targeting DNA and cell cycle. Neoplasia 9 830 PMID: 17971903
If you know of a relevant reference for Prazosin hydrochloride, please let us know.
关键词: Prazosin hydrochloride, Prazosin hydrochloride supplier, α1-adrenoceptor, alpha1-adrenoceptor, a1-adrenoceptor, antagonists, MT3, α1-adrenergic, alpha1-adrenergic, a1-adrenergic, Receptors, MT, Melatonin, cdk1, inactivation, inactivates, Adrenergic, Alpha-1, (MT), Alpha-2, 0623, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Prazosin hydrochloride 的部分引用包括:
Kahn et al (2016) The anti-hypertensive drug pra. inhibits glioblastoma growth via the PKCδ-dependent inhibition of the AKT pathway. EMBO Mol Med 8 511 PMID: 27138566
Skelly and Weiner (2014) Chronic treatment with pra. or dulox. lessens concurrent anxiety-like behavior and alcohol intake: evidence of disrupted noradrenergic signaling in anxiety-related alcohol use. Brain Behav 4 468 PMID: 25161814
Moura et al (2006) Alpha2-adrenoceptor subtypes involved in the regulation of catecholamine release from the adrenal medulla of mice. Br J Pharmacol 149 1049 PMID: 17075569
Delaney and Crane (2016) Presynaptic GABAB receptors reduce transmission at parabrachial synapses in the lateral central amygdala by inhibiting N-type calcium channels. Sci Rep 6 19255 PMID: 26755335
Zhu et al (2007) Tyramine excites rat subthalamic neurons in vitro by a DA-dependent mechanism. Neuropharmacology 52 1169 PMID: 17291545
Hughes et al (2013) Endogenous analgesic action of the pontospinal noradrenergic system spatially restricts and temporally delays the progression of neuropathic pain following tibial nerve injury. J Clin Invest 154 1680 PMID: 23707289
Zemkova et al (2011) NE causes a biphasic change in mammalian pinealocye membrane potential: role of alpha1B-adrenoreceptors, phospholipase C, and Ca2+. Endocrinology 152 3842 PMID: 21828176
Tjen-A-Looi et al (2011) Central and peripheral mechanisms underlying gastric distention inhibitory reflex responses in hypercapnic-acidotic rats. Am J Physiol Heart Circ Physiol 300 H1003 PMID: 21217073
Corcoran et al (2014) Dual effects of 5-HT(1a) receptor activation on breathing in neonatal mice. Pain 34 51 PMID: 24381267
Ajmo et al (2009) Blockade of adrenoreceptors inhibits the splenic response to stroke. Cell Rep 218 47 PMID: 19371742
Sjöblom et al (2001) Peripheral melatonin mediates neural stimulation of duodenal mucosal bicarbonate secretion. Exp Neurol 108 625 PMID: 11518737
Huang et al (2009) Repeated cocaine administration decreases 5-HT(2A) receptor-mediated serotonergic enhancement of synaptic activity in rat medial prefrontal cortex. Neuropsychopharmacology 34 1979 PMID: 19212317
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.