1、 s8Z, 8 U ,n(v “5 D S, Z 200032)K1: 胃动素主要在胃肠道表达,促进消化间期相收缩b而胃动素系统具体的作用机制尚未阐明,主要是因为缺乏对胃动素受体的了解b1999年Feighner等成功地鉴定和研究了胃动素受体的基因序列和生物学特性b这一重大发现促进了人们对胃动素系统的认识, 并对开发更加有效的胃肠动力药物提供了广阔的前景,为治疗临床大量胃肠动力性疾病将提供更有效的手段b本文就胃动素受体的研究进展作一综述b1oM: 胃动素; 受体; 胃肠动力ms |: R962 DS M : A cI|: 1001-0971(2001)06-0344-04 (motilin)
2、22 Ft, h (Vr, “hW M l Tb8 L , YVT % s87 t 8 H l bv = F 3 # 3( =)$ L s84,V7 B 5v bM s8Z ?C,+Y 1999 M s8 X Hk P 20 M “d | l Zb “d, 7? 0, v %h1 “5ilb1 s0 3+/ m 7,aC, Kb 3 S: Tt s8s9 L s8 %V , LV s8% ( BL)7d 7b ?Ct s8 1 *F,7 E=1 ,= 0 +, YVs cl(l8c% sF s8 L L?C8b8 L L # g M s8+sb, (“)a E=a ba (i s8,7?C s
3、8, s8 : E= b 8b s8sMb %V Hi s8Ya s8, O YaTMFb 8 V9 v f l ,4 U s8ibv ,1v s87, ?CT s84 ? v m Eb H8 s8 Lb1A L s8i,7 OVC iG l , ?$ E 9b s81 C *F,7 E=1 %bA Ud -i s8, -1i *F,1i F, 3N s8 T t,Bt s8 F4 Leu13,Phe3 s84,4 U s8 b4 s8t E= s8sc*l(l8s Fc% E=F, F s8 T ,VC0 +,4 Ui s8,NM4b5 ?1“ s8?1“ ,bDepoortere102 2
4、89 dt s8 LH l L,t s8 3* Vr, 3VCh gZ_ s8 /0b s8 “21? Hr, v/ Mt#345#SD0s 2001 M12 28 6 b7 r HWtla 9 HWBbLebenthal118l ? 3 H?C, 38 M, s8 i, , Mo(migrating motor complex, MMC)G 7i, MMCs) Ot e/b6 | MT s8|o b#b T ?t F125IS: ,i P V s8 9Fb3HS:?V , ?9Ft E= ? 3b 6BZ , cAMPY,GTPcAMP9FgTby7 .o YVG9F? 3, i= 0 db
5、12b8 = L L # T V$ a BJ1 * M“E,G = * t“d, O= 6 0Y Tb8 L5MQ, t 8H l T ?$aaa a t# , E, V$E4, T b T9X L Lb / 4 U,“ = 0 dbh GV 0 = , VN| 04adGVad 0G 0Yb8?C, VYVt 5 * s87 5 ,BVNO5t(VIP)b ya ? * s8 l T 5xb 4 UATPV ?9 1 *b MTL-R1A% H9VrNOSB1 *, VrYaM (Ya )B1y *13,4 U h 1y *,yX V ,NOS * 5 7y 14b7 s8 X Hk, “d
6、 3 T# M vwT,9 Fr 0 7?b “ - 5 ? %,Bb :(1) “ - 8v t dt s0 X H s8 L? 0 LTWw GPR38-AMTL-R1A,i TMTL-R1A 3 r b(2) LMTL-R1A B“ W%( *)Vr,i?C %Vrb58 = L L T1 YV * s8 LC, -8 L L T % b8 s8 LV , %OT(YVG ) ; % L9M,7 O ?E l rb L4 U %i s8bClark15 . , t t, s8 V ?i b ? %?CMTL-R1AmRNAVr,9 “ M1s8i V ? 16b(3) “dT s8.o
7、, “da“d1“ b#b(4) MTL-R1A haJFa (Vr, t 7 =i s8,t?C MTL-R1AY 8 t 2 T? (5)MTL-R1Ar1“Bb ID 1 McKeeKK, Tan CP, Palyha OC, et al. Cloning and cha-racterization of two human G protein-coupled receptor genes(GPR38 andGPR39) related tothegrowthhormonesecreta-gogue and neurotensin receptors J . Genomics, 1997
8、, 46(3) :426- 434.2 Feighner SD, Tan CP, McKee KK, et al. Receptor formotilin identified in the human gastrointestinal system J.Science, 1999, 284(5423) :2184- 2188.3 Miller P, Roy A, S-t Pierre S, et al. Motilin receptors inthe human antrum J . Am J Physiol Gastrointest LiverPhysiol, 2000, 278(1) :
9、G18- G23. 4 Miller P, Gagnon D, Dickner M, etal. Structure-functionstudies of motilin analoguesJ . Peptides, 1995, 16(1):#346# ForeignMedicalSciences SectiononPharmacy 2001 Dec; 28( 6)11- 18.5 Depoortere I, Thijs T, van Assche G, et al. Dose-depen-dent effects of recombinant human interleukin-11 on
10、con-tractile properties in rabbit 2, 4, 6-trinitrobenzene sulfonicacid colitis J. J Pharmacol Exp Ther, 2000, 294(3) :983- 990.6 Thielemans L, Depoortere I, Assche GV, et al. Demon-stration of a functional motilin receptor in TE671 cells fromhuman cerebellum J. Brain Res, 2001, 895( 1/2) :119- 128.7
11、 AlcaldeAI, PlazaMA, Marco R, et al. Study of the bind-ing of motilin to the membranes of enterocytes from rabbitjejunumJ . Peptides, 1996, 17(7) :1237- 1241.8 Poitras P, Miller P, Dickner M, et al. Heterogeneity ofmotilin receptors in the gastrointestinal tract of the rabbitJ. Peptides, 1996,17(4):
12、701- 707.9 SatohM, SakaiT, Sano I, etal. EM574, an erythromycinderivative, is a potent motilin receptor agonist in humangastric antrum J . J Pharmacol Exp Ther, 1994, 271(1):574- 579. 10 Depoortere I, Peeters TL, Vantrappen G, et al. Develop-ment of motilin receptors and of motilin- and erythromycin
13、-induced contractility in rabbits J. Gastroenterology,1990, 99( 3) :652- 658.11 Lebenthal A, Lebenthal E. The ontogeny of the small in-testinal epithelium J . J Parenter EnteralNutr, 1999, 23(5 Suppl): S3- S6.12 Depoortere I, Peeters TL. Transduction mechanism ofmotilin and motilides in rabbit duode
14、nal smooth muscleJ.Regul Pept, 1995, 55( 3) :227- 235.13 He XD, Goyal RK. Inhibitory junction potentials in themouse pyloric sphincter: roles of ATP, VIP and NO J.Gastroenterology, 1995, 108(4) :A975.14 PorterAJ, Wattchow DA, Brookers SJ, et al. The neuro-chemical coding and projections of circular
15、muscle motorneurons in the human colonJ . Gastroenterology, 1997,113(6) :1916- 1923.15 Clark MJ, Wright T, Bertrand PP, et al. Erythromycinderivatives ABT 229 andGM 611 act on motilin receptors inthe rabbit duodenum J . Clin Exp Pharmacol Physiol,1999, 26( 3) :242- 245.16 Pasricha P. Identifyingthem
16、otilin receptor: science, seren-dipity, or simply business J ? Gastroenterology, 1999,117(6) :1502- 1504. F )0Z9= ,1Z!8 f M ,n(= +Dv00 i, Z 200433)K1: 近年来抗真菌药物研究取得了很多进展,主要是发现了一些新的作用靶点和新的先导化合物b本文综述了作用于真菌细胞壁a抑制真菌蛋白质合成a抑制鞘脂生物合成和电子转移抑制剂四类新型抗真菌药物的作用机制和研究进展b1oM: 抗真菌药物ms |: R978.5 DS M : A cI|: 1001-0971(2
17、001)06-0347-05 ) Bnha?hb M “5 F 3 a 0 f4v ,)h #b 2MW, )h )h?h qv 6 1b“ - “5 F )0 v : )% 0( Ba B:aH wB:+1Mo) ) 0(5-J)b 7, B /7vvK ; B:H w B: l,l : 2001-05-08 3 007 P v; 5-J9i“ F ) Na? q5;7+1Mo ) rbyN “5 M1 7?raa F )0b M F )0 | vZ,BtToaT$?C,i 7? - “5b F )0TB8 b1 T )%C F )0 )%C F )0 #347#SD0s 2001 M12 28 6
