靶点的识别: Clinical trials 8. Comparison Participants a Safety E CLINICAL a Behavioral New Studies 点金 TRIALS星F actors 益8量8 Data Biomedical Medical Results Prospective Stages Benetits Monitoring Outsourced
靶点的识别: Clinical Trials 11
Classification of Drug Targets 核受体,2%其他,7% 核酸,2% 细胞膜受体, 离子通道, 45% 5% 细胞因子/激 素,11% 酶,28% 12
Classification of Drug Targets 12 细胞膜受体, 45% 酶, 28% 细胞因子/激 素, 11% 离子通道, 5 % 核酸, 2% 核受体, 2% 其他, 7%
受体( Receptors) 类型 药物活性 举例 Direct ligand-gated ion channel receptors GABAA receptors Barbiturate binding site Barbiturate agonists Benzodiazepine binding Benzodiazepines site agonists Acetylcholine receptors Nicotinic receptor evamisole agonists Nicotinic receptor Suxamethonium depolarizing antagonists Nicotinic receptor Galantamine allosteric modulators Glutamate receptors NMDA subtype Memantine (ionotropic) antagonists NMDA subtype Ketamine phencyclidine binding site antagonists
受 体（Receptors） 类型 药物活性 举例 Direct ligand-gated ion channel receptors GABAA receptors Barbiturate binding site agonists Barbiturate Benzodiazepine binding site agonists Benzodiazepines Acetylcholine receptors Nicotinic receptor agonists levamisole Nicotinic receptor depolarizing antagonists Suxamethonium Nicotinic receptor allosteric modulators Galantamine Glutamate receptors (ionotropic) NMDA subtype antagonists Memantine NMDA subtype phencyclidine binding site antagonists Ketamine Nature Reviews Drug Discovery, 2006, vol 5, 821
受体( Receptors) 类型 药物活性 举例 G-protein-coupled receptors Acetylcholine receptors Muscarinic receptor Pilocarpine agonists Muscarinic receptor Tropane derivatives antagonIsts Adenosine receptors Adenosine Al Caffeine receptor antagonIsts Theophylline Adrenoceptors agonists A noradrenaline, ephedrine ar-receptor antagonists Ergotamine a2-receptor, central Methyldopa agonists Br-receptor antagonists Propranolol, atenolol β2 receptor agonists Salbutamol Angiotensin receptors AT1- receptors antagonists Sartans
受 体 （Receptors） 类型 药物活性 举例 G-protein-coupled receptors Acetylcholine receptors Muscarinic receptor agonists Pilocarpine Muscarinic receptor antagonists Tropane derivatives Adenosine receptors Adenosine A1 receptor antagonists Caffeine Theophylline Adrenoceptors Agonists noradrenaline, ephedrine α1 -receptor antagonists Ergotamine α2 -receptor, central agonists Methyldopa β1 -receptor antagonists Propranolol, atenolol β2 -receptor agonists Salbutamol Angiotensin receptors AT1 -receptors antagonists Sartans Nature Reviews Drug Discovery, 2008, vol 5, 821
受体( Receptors) 类型 药物活性 举例 G-protein-coupled receptors Cysteinyl-leukotriene Antagonists Montelukast receptors Dopamine receptors Dopamine receptor Ropinirole subtype direct agonists pramipexole D,, D, and da antagonists Chlorpromazine, fluphenazine haloperidol GABAR receptors Agonists Baclofen Histamine receptors H1-antagonists Diphenhydramine 2-antagonists Cimetidine Opioid receptors H-opioid agonists Morphine, fentanyl opioid antagonists Naloxone K-opioid antagonists Buprenorphine
类型 药物活性 举例 G-protein-coupled receptors Cysteinyl-leukotriene receptors Antagonists Montelukast Dopamine receptors Dopamine receptor subtype direct agonists Ropinirole pramipexole D2 , D3 and D4 antagonists Chlorpromazine, fluphenazine, haloperidol GABAB receptors Agonists Baclofen Histamine receptors H1 -antagonists Diphenhydramine H2 -antagonists Cimetidine Opioid receptors μ-opioid agonists Morphine, fentanyl opioid antagonists Naloxone κ-opioid antagonists Buprenorphine Nature Reviews Drug Discovery, 2006, vol 5, 821 受 体 （Receptors）