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Prazosin

产品号 DB00457 公司名称 DrugBank
CAS号 19216-56-9 公司网站 http://www.ualberta.ca/
分子式 C19H21N5O4 电 话 (780) 492-3111
分子量 383.40114 传 真
纯 度 电子邮件 david.wishart@ualberta.ca
保 存 Chembase数据库ID: 340

产品价格信息

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产品别名

标题
Prazosin
IUPAC标准名
2-[4-(furan-2-carbonyl)piperazin-1-yl]-6,7-dimethoxyquinazolin-4-amine
IUPAC传统名
2-[4-(furan-2-carbonyl)piperazin-1-yl]-6,7-dimethoxyquinazolin-4-amine
商标名
Minipress
Minipress Xl
Vasoflex
Furazosin
Lentopres
别名
Prazosin Hydrochloride
Prazosin HCl
Prazocin
Prazosina [INN-Spanish]
Prazosine [INN-French]
Prazosinum [INN-Latin]

产品登记号

PubChem SID 46508594
PubChem CID 4893
CAS号 19216-56-9

产品性质

疏水性(logP) 1.3
溶解度 0.5 mg/mL (HCl salt) [Sigma Aldrich]

产品详细信息

详细说明 (English)
Item Information
Drug Groups approved
Description Prazosin is a selective α-1-adrenergic receptor antagonist used to treat hypertension. It has also been used to decrease urinary obstruction and relieve symptoms associated with symptomatic benign prostatic hyperplasia. α1-Receptors mediate contraction and hypertrophic growth of smooth muscle cells. Antagonism of these receptors leads to smooth muscle relaxation in the peripheral vasculature and prostate gland. Prazosin has also been used in conjunction with cardiac glycosides and diuretics in the management of severe congestive heart failure. It has also been used alone or in combination with β-blockers in the preoperative management of signs and symptoms of pheochromocytoma.
Indication For treatment of hypertension, symptomatic benign prostatic hyperplasia, and severe congestive heart failure. May also be used alone or in combination with β-blockers in the preoperative management of signs and symptoms of pheochromocytoma.
Pharmacology Prazosin is an alpha-adrenergic blocking agent used to treat hypertension and benign prostatic hyperplasia. Accordingly, Prazosin is a selective inhibitor of the alpha1 subtype of alpha adrenergic receptors. In the human prostate, Prazosin antagonizes phenylephrine (alpha1 agonist)-induced contractions, in vitro, and binds with high affinity to the alpha1c adrenoceptor, which is thought to be the predominant functional type in the prostate. Studies in normal human subjects have shown that Prazosin competitively antagonized the pressor effects of phenylephrine (an alpha1 agonist) and the systolic pressor effect of norepinephrine. The antihypertensive effect of Prazosin results from a decrease in systemic vascular resistance and the parent compound Prazosin is primarily responsible for the antihypertensive activity.
Affected Organisms
Humans and other mammals
Biotransformation Primarily hepatic. Several metabolites have been identified in humans and animals (6- O -demethyl, 7- O -demethyl, 2-[1-piperazinyl]-4-amino-6, 7-dimethoxyquinazoline, 2,4-diamino-6,7-dimethoxyquinazoline).
Absorption Well-absorbed from gastrointestinal tract; bioavailability is variable (50 to 85%).
Half Life 2-3 hours
Protein Binding 97%
Elimination Animal studies indicate that prazosin hydrochloride is extensively metabolized, primarily by demethylation and conjugation, and excreted mainly via bile and feces. Less extensive human studies suggest similar metabolism and excretion in man.
References
Bawaskar HS, Bawaskar PH: Utility of scorpion antivenin vs prazosin in the management of severe Mesobuthus tamulus (Indian red scorpion) envenoming at rural setting. J Assoc Physicians India. 2007 Jan;55:14-21. [Pubmed]
Cushman WC, Ford CE, Cutler JA, Margolis KL, Davis BR, Grimm RH, Black HR, Hamilton BP, Holland J, Nwachuku C, Papademetriou V, Probstfield J, Wright JT Jr, Alderman MH, Weiss RJ, Piller L, Bettencourt J, Walsh SM: Success and predictors of blood pressure control in diverse North American settings: the antihypertensive and lipid-lowering treatment to prevent heart attack trial (ALLHAT). J Clin Hypertens (Greenwich). 2002 Nov-Dec;4(6):393-404. [Pubmed]
Hiraoka Y, Taniguchi T, Tanaka T, Okada K, Kanamaru H, Muramatsu I: Pharmacological characterization of unique prazosin-binding sites in human kidney. Naunyn Schmiedebergs Arch Pharmacol. 2003 Jul;368(1):49-56. Epub 2003 Jun 25. [Pubmed]
Sigma Aldrich [Link]
External Links
Wikipedia
RxList
Drugs.com

参考文献

  • Sigma Aldrich Link
  • Bawaskar HS, Bawaskar PH: Utility of scorpion antivenin vs prazosin in the management of severe Mesobuthus tamulus (Indian red scorpion) envenoming at rural setting. J Assoc Physicians India. 2007 Jan;55:14-21. Pubmed
  • Cushman WC, Ford CE, Cutler JA, Margolis KL, Davis BR, Grimm RH, Black HR, Hamilton BP, Holland J, Nwachuku C, Papademetriou V, Probstfield J, Wright JT Jr, Alderman MH, Weiss RJ, Piller L, Bettencourt J, Walsh SM: Success and predictors of blood pressure control in diverse North American settings: the antihypertensive and lipid-lowering treatment to prevent heart attack trial (ALLHAT). J Clin Hypertens (Greenwich). 2002 Nov-Dec;4(6):393-404. Pubmed
  • Hiraoka Y, Taniguchi T, Tanaka T, Okada K, Kanamaru H, Muramatsu I: Pharmacological characterization of unique prazosin-binding sites in human kidney. Naunyn Schmiedebergs Arch Pharmacol. 2003 Jul;368(1):49-56. Epub 2003 Jun 25. Pubmed