红藻胶 | 9000-21-9

• 物质功能分类: 食品添加剂 - 增稠剂
• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 肉桂酸及其衍生物
• 中文名称: 红藻胶
• 中文别名: 1,4-二氢-2-甲基-6-苯基-4-(苯基乙炔基)-3,5-吡啶二甲酸3-乙基5-(苯基甲基)酯
• 英文名称: MRS-1191
• 英文别名: 3-Benzyl 5-ethyl 6-methyl-2-phenyl-4-(2-phenylethynyl)-1,4-dihydropyridine-3,5-dicarboxylate；5-O-benzyl 3-O-ethyl 2-methyl-6-phenyl-4-(2-phenylethynyl)-1,4-dihydropyridine-3,5-dicarboxylate
• CAS: 9000-21-9；185222-90-6
• 化学式: C₃₁H₂₇NO₄
• 分子量: 477.56
• InChiKey: SNVFDPHQAOXWJZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  6.1
• 重原子数：
  36
• 可旋转键数：
  9
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.16
• 拓扑面积：
  64.6
• 氢给体数：
  1
• 氢受体数：
  5

制备方法与用途

性质

红藻胶为白色至浅黄棕色粉末，无臭且味微咸。它易溶于75～77℃的水和牛奶中，形成坚实、光滑、有弹性的凝胶。1.5%的水分散液在37℃时产生粘度，在43℃达到最大值，超过此温度则粘度降低。红藻胶的质量即使经过数小时也不易下降，其凝胶与琼脂一样坚硬，并且比卡拉胶更为坚固。钾离子的存在会增加凝胶强度，而凝胶强度也随pH的变化而变化，pH为8时达到最高值，在低pH区域加热则降低。红藻胶不溶于乙醇。

用途

红藻胶用作增稠剂、粘接剂、稳定剂、胶凝剂和乳化剂。

使用范围

根据国家标准，建议红藻胶的添加量为千分之一到千分之三。

毒性

ADI未作特殊规定（FAO/WHO，2001）。可安全用于食品（FDA，§172.655，2000），大鼠经口LD₅₀为5000mg/kg。

使用限量

FAO/WH0 (1984, g/kg)：青刀豆和黄刀豆、甜玉米、蘑菇、芦笋、青豌豆等罐头产品中含奶油或其他油脂者为10；酪农干酪按稀奶油计为5；酸黄瓜为500mg/kg；肉汤、羹为5000mg/kg；胡萝卜罐头为10；发酵后经热处理的增香酸奶及其制品为5000mg/kg。

红藻胶还可用于牛奶布丁、牛奶冻、果酱、果冻和橘皮果冻、面包用果冻、冰淇淋、冰糕、乳蛋羹、掼奶油、洋火腿罐头、肉类及鱼类的贮藏、疗效食品等。

化学性质

红藻胶为白色至浅黄棕色粉末，无臭且味微咸。它易溶于75～77℃的水和牛奶中，形成坚实、光滑、有弹性的凝胶。1.5%的水分散液在37℃时产生粘度，在43℃达到最大值，超过此温度则粘度降低。红藻胶的质量即使经过数小时也不易下降，其凝胶与琼脂一样坚硬，并且比卡拉胶更为坚固。钾离子的存在会增加凝胶强度，而凝胶强度也随pH的变化而变化，pH为8时达到最高值，在低pH区域加热则降低。红藻胶不溶于乙醇。

生产方法

红藻胶由红藻类（Rhodophyceae）帚叉藻族（F“Mellar’in）的Fastigzata海藻在日光下晒干，然后用碱处理2～3周。经过中和、水洗、煮沸、抽提、离心分离后，在澄清液中添加1%的氯化钾溶液形成凝胶。将此凝胶于-16°C冷冻脱水，并在隧道式干燥机中于70℃下干燥，得率为原藻的2.5%～3.5%。红藻胶主要产自丹麦、挪威等国家海域。

反应信息

• 作为反应物：
  描述：

  红藻胶 在 四氯苯醌 作用下， 以 四氢呋喃 为溶剂， 反应 4.0h， 以74%的产率得到5-O-benzyl 3-O-ethyl 2-methyl-6-phenyl-4-(2-phenylethynyl)pyridine-3,5-dicarboxylate
  参考文献：
  名称：

  6-Phenyl-1,4-dihydropyridine Derivatives as Potent and Selective A₃ Adenosine Receptor Antagonists

  摘要：

  An approach to designing dihydropyridines that bind to adenosine receptors without binding to L-type calcium channels has been described. 1,4-Dihydropyridine derivatives substituted with beta-styryl or phenylethynyl groups at the 4-position and aryl groups at the 6-position were synthesized and found to be selective for human A(3) receptors. Combinations of methyl, ethyl, and benzyl esters were included at the 3- and 5-positions. Affinity was determined in radioligand binding assays at rat brain A(1) and A(2A) receptors using [H-3]-(R)-PIA [[H-3]-(R)-N-6-(phenylisopropyl)adenosine] and [H-3]CGS 21680 [[H-3]-2-[[4-(2-carboxymethyl)phenyl]ethylamino]-5'-(N-ethyl carbamoyl)adenosine], respectively. Affinity was determined at cloned human and rat A(3) receptors using [I-125]AB-MECA [N-6-(4-amino-3-iodobenzyl)-5'-(N-methycarbonyl)adenosine]. Structure-activity analysis indicated that substitution of the phenyl ring of the beta-styryl group but not of the 6-phenyl substituent was tolerated in A(3) receptor selective agents. Replacement of the 6-phenyl ring with a 3-thienyl or 3-furyl group reduced the affinity at A(3) receptors by 4- and g-fold, respectively. A 5-benzyl ester 4-trans-beta-styryl derivative, 26, with a K-i value of 58.3 nM at A(3) receptors, was >1700-fold selective vs either A(1) receptors or A(2A) receptors. Shifting the benzyl ester to the 3-position lowered the affinity at A(3) receptors 3-fold. A 5-benzyl, 3-ethyl ester 4-phenylethynyl derivative, 28, displayed a K-i value of 31.4 nM at A(3) receptors and 1300-fold selectivity vs A(1) receptors. The isomeric 3-benzyl, 5-ethyl diester was >600-fold selective for A(3) receptors. Oxidation of 28 to the corresponding pyridine derivative reduced affinity at A(3) receptors by 88-fold and slightly increased affinity at A(1) receptors.

  DOI：

  10.1021/jm960457c
• 作为产物：
  描述：

  苯丙炔醛 、 3-氧代-3-苯基丙酸苄酯 、 (E)-3-氨基巴豆酸乙酯 以 乙醇 为溶剂， 反应 24.0h， 以73 mg的产率得到红藻胶
  参考文献：
  名称：

  4-(苯基乙炔基)-6-苯基-1,4-二氢吡啶作为高选择性 A3 腺苷受体拮抗剂的结构-活性关系。

  摘要：

  4-(苯乙炔基)-6-苯基-1,4-二氢吡啶衍生物是人 A3 腺苷受体的选择性拮抗剂，与 [125I]AB-MECA (N6-(4-amino-3-碘苄基）-5'-（N-甲基氨基甲酰基）腺苷）在亚微摩尔范围内。在本研究中，综合探讨了二氢吡啶环不同位置（3-和5-酰基取代基、4-芳基取代基和1-甲基）的构效关系。利用1-乙氧基甲基和5-[2-(三甲基甲硅烷基)乙基]酯基团的联合保护，在5位形成游离羧酸，允许各种取代。确定新类似物对克隆人 A3 腺苷受体的选择性与大鼠脑 A1 和 A2A 受体上放射性配体的结合。腺苷受体的结构活性分析表明，4 位的吡啶基、呋喃基、苯并呋喃基和噻吩基最多只能对 A3 腺苷受体产生中等选择性。与4-苯乙烯基取代的二氢吡啶不同，4-苯乙炔基的环取代（例如4-硝基）没有提供增强的选择性。在二氢吡啶环的 3 位，酯对 A3 受体的选择性比密切相关的硫酯、酰胺和酮衍生物高得多。环状

  DOI：

  10.1021/jm970091j

文献信息

• 5-pyridyl-1, 3-azole compounds, process for producing the same and use there of
  申请人：Ohkawa Shigenori

  公开号：US20090048307A1

  公开（公告）日：2009-02-19

  An optionally N-oxidized compound represented by the formula: wherein R 1 represents hydrogen, hydrocarbon, heterocycle, amino, acyl, R 2 represents an aromatic group, R 3 represents hydrogen, pyridyl, aromatic hydrocarbon, X represents oxygen, optionally oxidized sulfur, Y represents a bond, an oxygen, optionally oxidized sulfur, a group represented by the formula NR 4 (R 4 represents hydrogen, hydrocarbon or acyl) and Z represents a bond or a divalent acyclic hydrocarbon, or a salt thereof has an excellent adenosine A 3 receptor antagonistic activity and is used as an agent for preventing or treating diseases related to an adenosine A 3 receptor. Furthermore, the compound (I) or a salt thereof has p38 MAP kinase inhibitory activity and TNF-α inhibitory activity and is used as an agent for preventing or treating diseases related to p38 MAP kinase and diseases related to TNF-α.

  一种可选择氧化的化合物，其化学式表示为：其中R1表示氢，碳氢化合物，杂环，氨基，酰基，R2表示芳香基团，R3表示氢，吡啶基，芳香烃，X表示氧，可选择氧化的硫，Y表示键，氧，可选择氧化的硫，一个由公式NR4（R4表示氢，碳氢化合物或酰基）表示的基团和Z表示键或二价无环碳氢化合物，或其盐具有出色的腺苷A3受体拮抗活性，并用作预防或治疗与腺苷A3受体相关的疾病的药剂。此外，该化合物（I）或其盐具有p38 MAP激酶抑制活性和TNF-α抑制活性，并用作预防或治疗与p38 MAP激酶和TNF-α相关的疾病的药剂。
• Modulation of the P2Y2 receptor pathway
  申请人：P2-Science APS

  公开号：EP2036567A2

  公开（公告）日：2009-03-18

  The present invention relates to the field of regulating the activity of the purinergic receptors for the modulation of the vascular tone, particularly for the purpose of treatment of haemodynamic conditions by overriding of vasoconstriction activity, such as increases in sympathic vasoconstriction. Modulators, such as UTP analogues as described herein are preferably specific for P2Y2. Compounds capable of stimulating the P2Y2 receptor are suitable for the treatment or prevention wherein inhibition of vasoconstriction activity is desirable such as hypertension and hypertension relates disorders or diseases, whereas compound capable of counteracting the activity of the P2Y2 receptor are suitable for the treatment of or prevention wherein inhibition of vasodilatation is desirable.

  本发明涉及调节嘌呤能受体活性以调节血管张力的领域，特别是通过抑制血管收缩活性（如交感血管收缩增加）来治疗血流动力学疾病。调节剂，如本文所述的UTP 类似物，最好对 P2Y2 具有特异性。能够刺激 P2Y2 受体的化合物适用于治疗或预防需要抑制血管收缩活性的疾病，如高血压和高血压相关失调或疾病，而能够抵消 P2Y2 受体活性的化合物适用于治疗或预防需要抑制血管舒张的疾病。
• Methods for reducing intraocular pressure
  申请人：——

  公开号：US20030153626A1

  公开（公告）日：2003-08-14

  A method for decreasing intraocular pressure by administering an A 3 subtype adenosine receptor antagonist, a calmodulin antagonist or an antiestrogen such as tamoxifen. These agents, by inhibiting influx or promoting efflux of aqueous humor, can be used to treat glaucoma.

  一种通过施用 A 3 亚型腺苷受体拮抗剂、钙调素拮抗剂或抗雌激素（如他莫昔芬）来降低眼压的方法。这些药物通过抑制房水的流入或促进房水的流出，可用于治疗青光眼。
• Purines are self-renewal signals for neural stem cells, and purine receptor antagonists promote neuronal and glial differentiation therefrom
  申请人：Goldman A. Steven

  公开号：US20050181503A1

  公开（公告）日：2005-08-18

  The present invention relates to a method of inhibiting differentiation of a population of neural stem cells by contacting a purinergic receptor agonist and a population of neural stem cells under conditions effective to inhibit differentiation of the population of neural stem cells. Another aspect of the present invention relates to a method of producing neurons and/or glial cells from a population of neural stem cells by culturing a population of neural stem cells with a purinergic receptor antagonist under conditions effective to cause the neural stem cells to differentiate into neurons and/or glial cells. The purinergic receptor agonist can also be used in a method of inducing proliferation and self-renewal of neural stem cells in a subject and a method of treating a neurological disease or neurodegenerative condition in a subject. The purinergic receptor antagonist can also be used in treating a neoplastic disease of the brain or spinal cord in a subject.

  本发明涉及一种抑制神经干细胞群体分化的方法，方法是在有效抑制神经干细胞群体分化的条件下，将嘌呤能受体激动剂与神经干细胞群体接触。本发明的另一方面涉及一种从神经干细胞群体中产生神经元和/或神经胶质细胞的方法，其方法是在有效促使神经干细胞分化成神经元和/或神经胶质细胞的条件下，用嘌呤能受体拮抗剂培养神经干细胞群体。嘌呤能受体激动剂还可用于诱导受试者神经干细胞增殖和自我更新的方法，以及治疗受试者神经系统疾病或神经退行性疾病的方法。嘌呤能受体拮抗剂还可用于治疗受试者的脑或脊髓肿瘤性疾病。
• 5-PYRIDYL-1,3-AZOLE COMPOUNDS, PROCESS FOR PRODUCING THE SAME AND USE THEREOF
  申请人：Takeda Pharmaceutical Company Limited

  公开号：EP1180518B1

  公开（公告）日：2007-01-17

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