CONESSINE

그림문자(GHS)

• 그림문자(GHS)

  

• 신호 어

  Warning

• 유해·위험 문구

  H315：피부에 자극을 일으킴

  H319：눈에 심한 자극을 일으킴

  H335：호흡 자극성을 일으킬 수 있음

• 예방조치문구

  P261：분진·흄·가스·미스트·증기·...·스프레이의 흡입을 피하시오.

  P264：취급 후에는 손을 철저히 씻으시오.

  P264：취급 후에는 손을 철저히 씻으시오.

  P271：옥외 또는 환기가 잘 되는 곳에서만 취급하시오.

  P280：보호장갑/보호의/보안경/안면보호구를 착용하시오.

  P302+P352：피부에 묻으면 다량의 물로 씻으시오.

  P305+P351+P338：눈에 묻으면 몇 분간 물로 조심해서 씻으시오. 가능하면 콘택트렌즈를 제거하시오. 계속 씻으시오.

CONESSINE 화학적 특성, 용도, 생산

• 개요

  Conessine is a naturally occurring steroid alkaloid found in a number of plant species from the Apocynaceae family, which have been used in traditional herbal medicine as a treatment for amoebic dysentery. In a radioligand-based high-throughput screen, conessine demonstrated high affinity for both rat and human histamine H3 receptors (K_is = 5.2 and 24.5 nM, respectively) and high selectivity against histamine receptors H1, H2, and H4. Though conessine potently blocks H3 agonist-stimulated GTPγS binding in cell- and tissue-based functional assays and efficiently crosses the blood-brain barrier, it has a poor rate of CNS clearance.

• 용도

  Conessine is a steroidal dibasic alkaloid with a rigid steroid-based skeleton. Conessine is a potent and selective histamine H3 receptor antagonist.

• 정의

  ChEBI: A steroid alkaloid that is con-5-enine substituted by a N,N-dimethylamino group at position 3. It has been isolated from the plant species of the family Apocynaceae.

• 생물학적 활성

  Potent and selective histamine H 3 receptor antagonist (pK i values are 7.61 and 8.27 at rat and human H 3 receptors respectively). A steroidal alkaloid that displays in vitro antiplasmodial activity (IC 50 = 1.04 μ M). Also has high affinity for α 2C adrenoceptors (pK i = 7.98).

• Purification Methods

  It crystallises from acetone, sublimes at 95o/0.01mm and boils at 0.1mm with bath temperature at 220o. The dihydrochloride has m >340o (browns at 235o and decomposes at 338-240o) and has [] D +9.3o (c 2, H2O). [Marshall & Johnson J Am Chem Soc 84 1458 1962, Beilstein 22 III/IV 4382.]

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