Hoi duge B13: THUOC GIAM DAU GAY NGHIEN, THUOC KICH THICH THAN KINH TRUNG ONG Tai ligu: 4. L8 Minh Tri, Huynh Thi Ngoc Phuong (2017). Héa Duge 1, NXB Gido Dye Vigt Nam 2. Truong Phugng, Tran Thanh Dao (2018). Héa dug 2 (Dung cho dae tao dug si dai hoc}, NXB Gido Duc Viet Nam. (trang 188-207, 216-247 ) 3. Thomas L. Lemke, David A. Williams et al. (2008). Foye's Principles of Medicinal Chemistry 7th edition, Wolter Kluwer. N@i dung: THUOC GIAM DAU GAY NGHIEN Bc diém chung opioid (central analgesic) - Pharmacora: 4-phenylpiperidin Tinh than dau cao - Nbc 3 N*, thung pKa 8-10 + SAR multicyclic opioid agonist & antagonist Multicyclic w agonists. $i 7 sox i @ ic | e" " Wo! Wo" o- ‘ 8 “ 2 My loRpMONE Morphine state hydration (Olu) oH cts KH @ CH ‘eG NH SH @ ro 4 ‘a Hyco T © oa cxymorphone 2 hydrochloride (Opana) Codeine sulfate Trln Thanh Mai 57Hod duge eH ° in 8 00) ¢ Hnfpon ‘ on woh Hyco" ° Coon ° 8 3 rocodone 1 Grycodene hystechiorde ) “iia troneodor 2 Mubticyelic x agonistsiu antaznnists. SHO © e He Wo" © x Nalbuphine hydrochloride (Nubain) Butorphitulticyclc opioid antagonists " gretlecne non O fon ‘o" of ‘e" Set Ba He! a ‘o. S 3 Naloxone hydrochloride: (Narcan) M4 Nscrs eo eo 12 Su Bio ne ha ‘. 3 Mothyinaltrexone bromide (Rosston Trin Thanh Mai 58Hoi duge 4 SAR flexible opioid (anilidopiperidin hay anilinopiperidin ) Flexible Opioids: Anilidopiperidines ig oHe Oly oF Anilidapiperidine ‘pharmacophore 9 cooH, Orgel Ch cook 6-0-0, ro-L2008 On OH OCH wo-Leao® ch tes ca @ yxe awe chy He oH) cH Poa Meperidine hydrachloride Fentanyl citrate Sufentanil ciate (Demerol (Subvimaze) {Sufonta} %e -CH:- CH oy Oy CH sa Hols 4 oe CH Ce: FE ‘OCH: a Alfentanil hydrochloride Remifentanil hydrochloride Methadone hydrochloride (Alfenta) (Utiva} (Dolophine) Flexible jp agonists, 1D Morphin hydreclorid : Ci7HisNOs HCI. 3H20) Ptl: 375.8 ~ Tan: (4R4aR,7S,7aR,120S}-3-methy!-2,4,4a,7,7a,13-hexahydro-1H-4,12-methanobenzafura[a,2- sJisoquinoline-7,9.diol;hydrochloride Trin Thanh Mai 59Hod dug cr Awcu @ Ho HO" ‘ 3H.0 Sy THUOC KICH THICH TKTW Thuéc kich thich TKTW thuéng phan loal theo tac dung dugc ly chon loc, phan theo cu tric thi cé nhiéu nhém: = Xanthin: caffein, (theophyllin, theobromin) = Phenyllalkylamin: phenyllethylamin, phenyllisopropylamin (amphetamin, - Indolalkylamine = Alkaloid thién nhién: strychnin, cocain, .. Nhém xanthin ~ Caffein (1,3,7-trimethyl xanthin) -Theophyllin (1,3-dimethy! xanthin) = Theobromin (3,7-dimethyl xanthin) g 4 weg A a Huey nae Catraine Theophylline Theobromine Trin Thanh Mai 60Hod duge © Nhém xanthin: de ° HG Wo oan nope My NO Hco,tiH,O ott Se — L v cH, ELOH oF sn nm, PACD i oy i 1a-cimenyures ethyl 2eyanoscetate 1a-gimetyttanine- Smeaoursel 3 ° ° 9 Wea, NH Hie ; NH, (CHISO, | HC. ‘ May ee ee fi f wm) ONY oy oy by om om em Lamethpsscmino- 1 gdimethytanine- treephtine catuine ree lormartnowraeh Nhém xanthin: tinh chét chung anh MaiHoi drge Q Caffein CaHicNeO: 194.19 = Tén: 1,3,7-trimethylpurine-2,6-dione Q Thoophyitin CrHaNsOz 180.16 = Tén: 1,3-dimethyl-7H-purine-2,6-dione Trin Thanh MaiHod dirge Phenylisopropylamine Stimulants: Amphetamine- Related Agents /NHe NH NH-CaHs CF, S{+)Amphetamine — p-Chloroamphetamine = Fenfluramine (PCA) % SAR phenylalkylamin - pheylisopropylamin 2 Amphetamine CoHsaN 135.21 = 1-phenylpropan-2-amine Q Strychnin Trlin Thanh Mai 63