Apomorphine

• 产品号: DB00714
• CAS号: 41372-20-7
• 分子式: C17H17NO2
• 分子量: 267.32238

产品别名

• 标题: Apomorphine
• IUPAC标准名: (9R)-10-methyl-10-azatetracyclo[7.7.1.0^{2,7}.0^{13,17}]heptadeca-1(16),2(7),3,5,13(17),14-hexaene-3,4-diol
• IUPAC传统名: apomorphine
• 商标名: Ixense; Uprima; Apokyn
• 别名: VR004; Apomorphine Hydrochloride Hemihydrate; VR-400; L-Apomorphine; Apomorfin; Apomorphinium Chloride Hemihydrate; Apormorphine; apomorphine; VR-040; Apomorphine Hydrochloride

产品登记号

• PubChem CID: 6005
• CAS号: 41372-20-7
• PubChem SID: 46508653

产品性质

• 疏水性(logP): 3.1
• 溶解度: 1.66E+004 mg/L

产品详细信息

详细说明 (English)

• Drug Groups: approved; investigational
• Description: A derivative of morphine that is a dopamine D2 agonist. It is a powerful emetic and has been used for that effect in acute poisoning. It has also been used in the diagnosis and treatment of parkinsonism, but its adverse effects limit its use. [PubChem]
• Indication: For the acute, intermittent treatment of hypomobility, off episodes (end-of-dose wearing off and unpredictable on/off episodes) associated with advanced Parkinson's disease.
• Pharmacology: Apomorphine is a type of dopaminergic agonist, a morphine derivative which primarily affects the hypothalamic region of the brain. Drugs containing this substance are sometimes used in the treatment of Parkinson's disease or erectile dysfunction. In higher doses it is a highly effective emetic.
• Toxicity: LD₅₀=0.6 mmoles/kg (mice, intraperitoneal)
• Affected Organisms: Humans and other mammals
• Biotransformation: Hepatic
• Absorption: 100% following subcutaneous administration
• Half Life: 40 minutes (range 30 - 60 minutes)
• Protein Binding: ~50%-albumin
• Distribution: * 123 to 404 L
• Clearance: * 223 L/hr
• References: Matsumoto K, Yoshida M, Andersson KE, Hedlund P: Effects in vitro and in vivo by apomorphine in the rat corpus cavernosum. Br J Pharmacol. 2005 Sep;146(2):259-67. [Pubmed] ; SCHWAB RS, AMADOR LV, LETTVIN JY: Apomorphine in Parkinson's disease. Trans Am Neurol Assoc. 1951;56:251-3. [Pubmed] ; Cotzias GC, Papavasiliou PS, Fehling C, Kaufman B, Mena I: Similarities between neurologic effects of L-dipa and of apomorphine. N Engl J Med. 1970 Jan 1;282(1):31-3. [Pubmed] ; Corsini GU, Del Zompo M, Gessa GL, Mangoni A: Therapeutic efficacy of apomorphine combined with an extracerebral inhibitor of dopamine receptors in Parkinson's disease. Lancet. 1979 May 5;1(8123):954-6. [Pubmed] ; Chaudhuri KR, Clough C: Subcutaneous apomorphine in Parkinson's disease. BMJ. 1998 Feb 28;316(7132):641. [Pubmed]
• External Links: Wikipedia; RxList; Drugs.com

参考文献

• Matsumoto K, Yoshida M, Andersson KE, Hedlund P: Effects in vitro and in vivo by apomorphine in the rat corpus cavernosum. Br J Pharmacol. 2005 Sep;146(2):259-67. Pubmed
• SCHWAB RS, AMADOR LV, LETTVIN JY: Apomorphine in Parkinson's disease. Trans Am Neurol Assoc. 1951;56:251-3. Pubmed
• Cotzias GC, Papavasiliou PS, Fehling C, Kaufman B, Mena I: Similarities between neurologic effects of L-dipa and of apomorphine. N Engl J Med. 1970 Jan 1;282(1):31-3. Pubmed
• Corsini GU, Del Zompo M, Gessa GL, Mangoni A: Therapeutic efficacy of apomorphine combined with an extracerebral inhibitor of dopamine receptors in Parkinson's disease. Lancet. 1979 May 5;1(8123):954-6. Pubmed
• Chaudhuri KR, Clough C: Subcutaneous apomorphine in Parkinson's disease. BMJ. 1998 Feb 28;316(7132):641. Pubmed