药理学绪论:药理学英文课件.ppt

  1. 1、本文档共153页,可阅读全部内容。
  2. 2、本文档内容版权归属内容提供方,所产生的收益全部归内容提供方所有。如果您对本文有版权争议,可选择认领,认领后既往收益都归您。
  3. 3、本文档由用户上传,本站不保证质量和数量令人满意,可能有诸多瑕疵,付费之前,请仔细先通过免费阅读内容等途径辨别内容交易风险。如存在严重挂羊头卖狗肉之情形,可联系本站下载客服投诉处理。
  4. 文档侵权举报电话:400-050-0739(电话支持时间:9:00-19:00)。
Antagonist拮抗药 Competitive antagonist 竞争性拮抗药 Ligand (L) Inhibitor(I) [RT] = [R] + [LR] + [IR] [LR]/[RT] = [L]/KD + [L] [LR]/[RT] = [L]/[L] + KD(1 + [I]/KI) Competitive Antagonist 药物的作用取决于 [I]/KI, [I]浓度愈高或KI愈小,激动药的效应低, 拮抗作用强。 如果[LR]/[RT]→100%, 激动药的量效 反应曲线可以被竞争性拮抗药平行右移。 如果增加竞争性激动药浓度,仍可达到 Emax. Competitive Antagonist(A) 激动药的量效反应曲线被竞争性拮抗药平行右移, 如果增加竞争性激动药浓度,仍可达到Emax。 Competitive Antagonist(A) 激动药的量效反应曲线被竞争性拮抗药平行右移, 如果增加竞争性激动药浓度,仍可达到Emax。 Competitive Antagonist pA2 is the antagonism parameter pA2 = -log[I] = -logKI pA2 Express the extent of antagonism of a given antagonist, when the agonist and antagonist are used in same preparation, two times concentration (X2) of agonist(A2) only produce ordinary concentration of that agonist effect, in that time the negative log concentration of antagonist is called as pA2 . B. Noncompetitive antagonist 非竞争性拮抗药 Spare receptors ( by Stephenson 1956) 储备受体 Uncompetitive Antagonist(B) 激动药的量效反应曲线不能被非竞争性拮抗药平行右移,如果增加激动药浓度,不能达到Emax。 5. The Types of Receptors According to protein structure, transmembrane signaling mechanisms, effect properties and sites of receptors, the classifications of receptors as follows: The Types of Receptors (1) G protein coupling receptors (G-蛋白偶联受体) Gs, Gi, Gt(transducin), Go α,β, D, 5-HT, M, Opioid, Purine, PG 受体 Types of Receptors (2) Ligand-gated ion channel receptors (配体门控离子通道受体, receptors containing ion channel) N, GABA receptors Ach + N2 receptor → Na+ channel open → depolarization → skeletal muscle contraction. Types of Receptors (3) Tyrosine protein kinase receptors (酪氨酸激酶活性受体) Insulin(胰岛素) Epidermal growth factor(上皮生长因子, EGF) Platelet-derived growth factor (血小板衍生的生长因子, PDGF) Transforming growth factor-β (转化生长因子β, TGF-β) Insulin-like growth factor(胰岛素样生长因子) Types of Receptors (4) Intracellular receptors (细胞内受体) Cor

文档评论(0)

共享文档
该用户很懒,什么也没介绍

相关文档

相关课程推荐