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摘要: 下尿路储尿和排尿功能主要由脊髓反射和脊上神经中枢介导。许多研究表明5-羟色胺(5-HT)受体对调节这两个通路均有显著作用,其中尤以5-HT1A受体为甚,其次为5-HT2、5-HT3和5-HT7受体。5-HT2受体分为5-HT2A、5-HT2B、5-HT2C三种亚型,其中对排尿有影响的主要为5-HT2A、5-HT2C这两种亚型。本文主要就5-HT2受体的结构、分布、药理作用以及5-HT2受体对排尿影响的研究进展作一综述。
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[1] KELLY A B, CLARKE W P, CUNNINGHAM K A, et al. Fine-tuning serotonin2c receptor function in the brain:molecular and functional implications[J]. Neuropharmacoloy, 2008, 55:969-976.
[2] BERG K A, HARVEY J A, SPAMPRINATO U, et al. Physiological and therapeutic relevance of constitutive activity of 5-HT2A and 5-HT2C receptors for the treatment of depression[J]. Prog Brain Res, 2008, 172:287-305.
[3] KROEZE W K, KRISTIANSEN K, ROTH B L. Molecular biology of serotonin receptors structure and function at the molecular level[J]. Curr Top Med Chem, 2002, 2:507-528.
[4] LEYSEN J E. 5-HT2 Receptors[J]. Curr Drug Targets CNS Neurol Disord, 2004, 3:11-26.
[5] XU C, GIULIANO F, SUN X Q, et al. Serotonin 5-HT2A and 5-HT5A receptors are expressed by different motoneuron populations in rat Onuf's nucleus[J].J Comp Neurol,2007,502:620-634.
[6] BREA J, CASTRO-PALOMINO J, YESTE S, et al. Emerging opportunities and concerns for drug discovery at serotonin 5-HT2B receptors[J]. Curr Top Med Chem, 2010, 10:493-503.
[7] KENNETT G A, WOOD M D, BRIGHT F, et al. SE 242084, a selective and brain penetrant 5-HT2C receptor antagonist[J]. Neuropharmacology,1997, 36:609-620.
[8] DOWD C S, HERRICK-DAVIS K, EGAN C, et al. 1-[4-(3-Phenylalkyl)phenyl]-2-aminopropanes as 5-HT2A) partial agonists[J]. J Med Chem, 2000, 43:3074-3084.
[9] VAN OEKELEN D, MEGENS A, MEERT T. Functional study of rat 5-HT2A receptors using antisense oligonucleotides[J]. J Neurochem, 2003, 85:1087-1100.
[10] JENSEN N H, CREMERS T I, SOTTY F, et al. Therapeutic potential of 5-HT2C receptor ligands[J].Scientific World Journal, 2010,10:1870-1885.
[11] ANDREW M D, FISH P V, BLAGG J, et al. Pyrimido[4,5-d] azepines as potent and selective 5-HT2C receptor agonists:Design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence[J]. Bioorg. Med Chem Lett, 2010, 21:2175-2720.
[12] LEE J, JUNG L M, LEE J H. 5-HT2C receptor modulators:a patent survey[J]. Expert Opin Ther Pat, 2010, 20:1429-1455.
[13] DOLY S, MADEIRA A, FISCHER J, et al. The 5-HT2A receptor is widely distributed in the rat spinal cord and mainly localized at the plasma membrance of postsynaptic neurons[J]. J Comp Neurol, 2004, 472(2):496-511.
[14] ZENG F Q, XU C, XU G. Distribution of serotonin 5-HT2A and 5-HT7 receptors in the Onuf's nucleus of the rat spinal cord[J]. Neural Regen Res, 2008, 3(8):853-857.
[15] STEERS W D, DE GROAT W C. Effects of mchlorophenylpiperazine on penile and bladder function in rats[J]. Am J Physiol, 1989, 257:R1441-R1449.
[16] GUARNERI L, IBBA M, TESTA R, et al. The effects of mCPP on bladder voiding contractions in rats are mediated by the 5-HT2A/5-HT2C receptors[J]. Neurourol Urodyn,1996,15:316-317(abstracts).
[17] DE GROAT W C. Influence of central serotonergic mechanisms on lower urinary tract function[J]. Urology, 2002, 9(5 Suppl 1):30-36.
[18] TESTA R, GUARNERI L, ANGELIC P. Effect of different 5-hydroxytryptamine receptor subtype antagonists on the micturition reflex in rats[J]. Br J Urol Int,2001,87:256-264.
[19] DANUSER H, THOR K B. Spinal 5-HT2 receptor-mediated facilitation of pudendal nerve reflexes in the anaesthetized cat[J]. Br J Pharmacol,1996,118:150-154.
[20] MCNURRAY G, MINER W D. The effect of the 5-HT2C agonist Ro600175 on urinary cystometric parameters in the guinea pig[J]. FASEB,2005,19:Abstract #320.3.
[21] CONLON K, MINER W, MCCLEARY S, et al. Identification of 5-HT2C mediated mechanisms involved in urethral sphincter reflexes in a guinea-pig model of urethral function[J]. BJU International, 2011:1464-146x.
[22] MBAKI Y, WESTBROOK S L, RAMAGE A G.The role of 5-HT2 receptors subtypes in the control of the urethra and micturition in anaesthetized female rats[J]. Proceeding of BPS meeting December 2005 UCL London.
[23] MBAKI Y, RAMAGE A G. Investigation of the role of 5-HT2 receptor subtypes in the control of the bladder and the urethra in the anaesthetized female rat[J]. 2008,155:343-356.
[24] MBAKI Y, RAMAGE A G, MCNURRAY G, et al. 5-HT2A receptor activation of the external urethral sphincter and 5-HT2C receptor inhibition of micturition:A study based on pharmacokinetics in the anaesthetized female rat[J]. Eur J Pharmacol, 2012, 682:142-152.
[25] KADEKAWA K, NISHIJIMA S, SUGAYA K, et al. Mechanisms by which the serotonergic system inhibits micturition in rats[J]. Life Sci, 2009, 85:592-596.
[26] ISHIZUKA O, GU B J, IGAWA Y, et al. Role of supraspinal serotonin receptors formicturition in normal conscious rats[J]. Neurourol Urodyn,2002,21:225-230.
[27] CORSI M, TOSON P G, PIETRA G, et al. Pharmacological analysis of 5-hydroxytryptamine effects on electrically stimulated human isolated urinary bladder[J]. Br J Pharmacol,1991,104:719-725.
[28] MESSORI E, RIZZI C A, CANDURA S M, et al. 5-Hydroxytryptamine receptors that facilitate excitatory neuromuscular transmission in the guinea-pig isolated detrusor muscle[J]. Br J Pharmacol, 1995, 115:677-683.
[29] REKIK M, LLUEL P, PALEA S. 5-Hydroxytr-yptamine potentiates neurogenic contractions of rat isolated urinary bladder through both 5-HT7 and 5-HT2C receptors[J]. Eur J Pharmacol,2011,650:403-410.
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