ASSESSMENT OF THE EFFECTS OF TOPICAL ADMINISTRATION OF CHEMODENERVATING PHARMACEUTICALS
    3.
    发明公开
    ASSESSMENT OF THE EFFECTS OF TOPICAL ADMINISTRATION OF CHEMODENERVATING PHARMACEUTICALS 审中-公开
    测试效果局部给药化学DENERVIERENDER制药

    公开(公告)号:EP2015773A2

    公开(公告)日:2009-01-21

    申请号:EP07861297.5

    申请日:2007-04-27

    申请人: Anterios, Inc.

    发明人: EDELSON, Jonathan

    IPC分类号: A61K39/02

    摘要: The present invention provides methods for assessing the activity of topically administered chemodenervating agents. In some embodiments, methods for assessing the activity of topically administered chemodenervating agents involve determining the extent of inhibition of acetylcholine release near the site of administration. In some embodiments, methods for assessing activity of topically administered chemodenervating agents involve observing a reflex motion of a limb of a subject.

    ALLOSTERIC SITES ON MUSCARINIC RECEPTORS
    6.
    发明公开
    ALLOSTERIC SITES ON MUSCARINIC RECEPTORS 审中-公开
    变构部位ON MUSACARIN受体

    公开(公告)号:EP1222463A2

    公开(公告)日:2002-07-17

    申请号:EP00971543.4

    申请日:2000-10-20

    IPC分类号: G01N33/566 A61K31/395

    摘要: An allosteric site on muscarinic receptors is disclosed, together with its use for screening for compounds capable of modulating the binding of a primary ligand such as acetylcholine to the receptor. The site is characterised herein a series of indolocarbazoles represented by formula (1) and a series of related compounds represented by formula (2). These compounds are capable of binding to the allosteric site to modulate the binding of a primary ligand to the receptors, showing positive, negative and neutral cooperativity and selectivity for muscarinic receptor subtypes.

    ALPHA O-SUPERFAMILY CONOTOXIN PEPTIDE, PHARMACEUTICAL COMPOSITION AND USE THEREOF
    9.
    发明公开
    ALPHA O-SUPERFAMILY CONOTOXIN PEPTIDE, PHARMACEUTICAL COMPOSITION AND USE THEREOF 审中-公开
    α-O超家族内毒素多肽,药物组合物及其用途

    公开(公告)号:EP2889308A1

    公开(公告)日:2015-07-01

    申请号:EP13804082.9

    申请日:2013-06-08

    申请人: Hainan University

    摘要: The present invention pertains to fields of biochemistry and molecular biology, relates to an αO-superfamily conotoxin peptide, pharmaceutical composition thereof, preparation method and use thereof. The present invention further relates to a propeptide of the conotoxin peptide, nucleic acid construct thereof, expression vector and transformed cell thereof, and fusion protein thereof. The present invention further relates to a method for blocking acetylcholine receptors as well as a use of the conotoxin peptide in the manufacture of a medicament. The new αO-superfamily conotoxin peptide of the present invention is capable of specifically blocking acetylcholine receptor (nAChRs) (e.g., α9α10 nAChR), and NMDA receptor (e.g., NR2C NMDAR), and has activity for treatment of neuralgia, addiction, and activity for treatment of chemotherapy of cancers, breast cancer, lung cancer, wound healing, epilepsia, ischemia, and thus is promising in the manufacture of analgesic, a medicament for treatment of addiction, and a tool drug for neuroscience.

    摘要翻译: 本发明涉及生物化学和分子生物学领域,涉及一种αO超家族芋螺毒素肽,其药物组合物及其制备方法和用途。 本发明还涉及芋螺毒素肽的前肽,其核酸构建体,表达载体及其转化细胞及其融合蛋白。 本发明进一步涉及阻断乙酰胆碱受体的方法以及芋螺毒素肽在制造药物中的用途。 本发明的新型αO超家族芋螺毒素肽能够特异性阻断乙酰胆碱受体(nAChR)(例如α9α10nAChR)和NMDA受体(例如NR2C NMDAR),并且具有治疗神经痛,成瘾和活性的活性 用于治疗癌症,乳腺癌,肺癌,伤口愈合,癫痫,局部缺血的化学疗法,因此在制造止痛剂,治疗成瘾药物和神经科学用工具药物方面是有前景的。

    QUANTIFICATION OF BOTULINUM TOXIN
    10.
    发明授权
    QUANTIFICATION OF BOTULINUM TOXIN 无效
    肉毒杆菌毒素的定量

    公开(公告)号:EP1597584B1

    公开(公告)日:2007-11-14

    申请号:EP04713111.5

    申请日:2004-02-20

    申请人: Ipsen Limited

    IPC分类号: G01N33/68 G01N33/94 G01N33/50

    CPC分类号: G01N33/944 G01N33/5088

    摘要: The invention relates to a method for determining the quantity of pre-synaptic neuromuscular blocking substance (notably botulinum toxin) contained in a sample. In one aspects, the method comprises the following steps: (i) determining the minimum voltage Vm needed to induce the contraction of muscle tissue, said muscle tissue being connected to an electrical stimulator through a motor nerve and preferably immersed in an oxygenated physiological buffer containing glucose; (ii) adding the sample containing the pre-synaptic neuromuscular blocking substance; (iii) electrically stimulating, at a voltage at least equal to Vm, the muscle tissue at certain time intervals; (iv) comparing the effect induced by the sample to the effect induced by a reference substance and thereby determining the quantity of the pre-synaptic neuromuscular blocking substance in the sample.