CAS: 298-45-3; Bulbocapnine

该化合物是一种自然产生的藻类,产自Corydalis和Dentra基因植物,其特征为脱氧代谢对应形式,并研究其药理特性,特别是多巴胺受体敌;该化合物明显地与D1和D2多巴胺受体结合,使其成为...

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CAS号552-29-4 oxyhydrastinine

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    📜6,7,7A,8-四氢-11-甲氧基-7-甲基-5H-苯并(G)-1,3-苯并二氧杂环戊烯并(6,5,4-De)喹啉-12-醇置于d-酒石酸体系中,化学反应生成空褐麟碱
    参考文献:Kikkawa,Yakugaku Zasshi/journal Of The Pharmaceutical Society Of Japan,1959,Vol. 79,P. 1244,1247
    标题:Kikkawa,Yakugaku Zasshi/journal Of The Pharmaceutical Society Of Japan,1959,Vol. 79,P. 1244,1247

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    专利信息


    专利号:US-2004101523-A1
    优先权日:1989-07-27
    标题:Renal-selective prodrugs for control of renal smpathetic nerve activity in the treatment of hypertension
    发明人:REITZ DAVID B; KOEPKE JOHN P; BLAINE EDWARD H; SCHUH JOSEPH R; MANNING ROBERT E; SMITS GLENN J
    权利人:SEARLE & CO
    摘要:Renal-selective prodrugs are described which are preferentially converted in the kidney to compounds capable of inhibiting synthesis of catecholamine-type neurotransmitters involved in renal sympathetic nerve activity. The prodrugs described herein are derived from inhibitor compounds capable of inhibiting one or more of the enzymes involved in catecholamine synthesis, such compounds being classifiable as tyrosine hydroxylase inhibitors, or as dopa-decarboxylase inhibitors, or as dopamine-β-hydroxylase inhibitors. These inhibitor compounds are linked to a chemical moiety, such as a glutamic acid derivative, by a cleavable bond which is recognized selectively by enzymes located predominantly in the kidney. The liberated inhibitor compound is then available in the kidney to inhibit one or more of the enzymes involved in catecholamine synthesis. Inhibition of renal catecholamine synthesis can suppress heightened renal nerve activity associated with sodium-retention related disorders such as hypertension. Conjugates of particular interest are glutamyl derivatives of dopamine-β-hydroxylase inhibitors, of which N-acetyl-γ-glutamyl fusaric acid hydrazide (shown below) is preferred.

    专利号:WO-9201667-A1
    优先权日:1990-07-25
    标题 :Renal-selective prodrugs for control of renal sympathetic nerve activity in the treatment of hypertension
    发明人:REITZ DAVID B; KOEPKE JOHN P; BLAINE EDWARD H; SCHUH JOSEPH R; MANNING ROBERT E; SMITS GLENN J
    权利人:SEARLE & CO
    摘要:Renal-selective prodrugs are described which are preferentially converted in the kidney to compounds capable of inhibiting synthesis of catecholamine-type neurotransmitters involved in renal sympathetic nerve activity. The prodrugs described herein are derived from inhibitor compounds capable of inhibiting one or more of the enzymes involved in catecholamine synthesis, such compounds being classifiable as tyrosine hydroxylase inhibitors, or as dopa-decarboxylase inhibitors, or as dopamine-β-hydroxylase inhibitors. These inhibitor compounds are linked to a chemical moiety, such as a glutamic acid derivative, by a cleavable bond which is recognized selectively by enzymes located predominantly in the kydney. The liberated inhibitor compound is then available in the kidney to inhibit one or more of the enzymes involved in catecholamine synthesis. Inhibition of renal catecholamine synthesis can suppress heightened renal nerve activity associated with sodium-retention related disorders such as hypertension. Conjugates of particular interest are glutamyl derivatives of dopamine-β-hydroxylase-inhibitors, of which N-acetyl-η-glutamyl fusaric acid hydrazide [represented in formula (a)] is preferred.

    专利号:US-11806326-B2
    优先权日:2018-01-29
    标 题 :Methods for dopamine modulation in human neurologic diseases
    发明人:SACKNER-BERNSTEIN JONATHAN
    权利人:SACKNER BERNSTEIN JONATHAN
    摘要:A method of treating Parkinson's Disease, Huntington's Disease and the like, diseases with abnormal dopamine-neuro-transmission, using small molecules administered systemically that penetrate into the central nervous system to inhibit the rate-limiting step of dopamine synthesis in the central nervous system, the conversion of L-tyrosine to L-3, 4-dihydroxyphenylalanine (L-DOPA) by tyrosine hydroxylase along with its cofactors tetrahydrobiopterin and iron (Fe+).

    专利号:US-4285938-A
    优先权日:1979-10-11
    标 题:7,8-Dihydroxy-1-(sulfamylphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepine derivatives
    发明人:PFEIFFER FRANCIS R
    权利人:SMITHKLINE CORP
    摘要:New 7,8-dihydroxy-1-(sulfamylphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepines having pharmaceutical activity together with new intermediates and methods of synthesis for preparing them. The lead compound is 6-chloro-7,8-dihydroxy-1-(p-sulfamylphenyl)-2,3,4,5-tetrahydro-1H-3-be nzazepine which has very potent renal dopaminergic activity.

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    ✅ COA系统入驻 | 共享模式

    合成参考文献


    摘要:STERN P, MITROVIC-KOCIC D. [Pharmacological analysis of bulbocapnine-induced catalepsy in the mouse]. Arch Int Pharmacodyn Ther. 1958 Sep 01;116(3-4):489–98.
    摘要:BOSWART J, BLAZEK Z. [Colorimetric determination of bulbocapnine]. Cesk Farm. 1954 Jun;3(6):200–3.
    参考文献:10.1254/jjp.3.149
    摘要:HARA S, KAWAMORI K. Pharmacological studies on the function of the extrapyramidal system. 2. Mechanism of the appearance of tremor due to extrapyramidal poisons. Jpn J Pharmacol. 1954 Mar;3(2):149–56. doi: 10.1254/jjp.3.149.
    参考文献:10.1007/bf00499902
    摘要:Jackisch R, Moll S, Feuerstein TJ, Hertting G. Dopaminergic modulation of hippocampal noradrenaline release. Evidence for alpha 2-antagonistic effects of some dopamine receptor agonists and antagonists. Naunyn Schmiedebergs Arch Pharmacol. 1985 Aug;330(2):105–13. doi: 10.1007/bf00499902.
    参考文献:10.1007/bf02158347
    摘要:Shamma M. The conformation of 4.5-substituted aporphine alkaloids. Cellular and Molecular Life Sciences. 1960 Nov;16(11):484–5. doi: 10.1007/bf02158347.
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