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1991 | 42 | 1 |

Tytuł artykułu

Serotonin receptors and site-selective agents

Autorzy

Treść / Zawartość

Warianty tytułu

Języki publikacji

EN

Abstrakty

EN
Few site-selective serotonergic agents are currently available; in fact, most of these agents might more appropriately be termed semi-selective in that they typically bind to at least two different populations of serotonin receptors. We describe the application of structure-affinity relationship (SAFIR) studies to the development of high- affinity and/or site-selective serotonergic agents; examples are provided from work conducted in our laboratories. Also discussed is the concept of selectively non-selective agents and their potential preclinical and clinical utility. A case is made for development of selective and nonselective serotonergic agents.

Wydawca

-

Rocznik

Tom

42

Numer

1

Opis fizyczny

p.49-60,fig.,ref.

Twórcy

  • Department of Medicinal Chemistry, School of Pharmacy, Medical College of Virginia, Virginia Commonwealth University, Richmond, Virginia 23298-0540, USA

Bibliografia

  • 1. Glennon RA, Westkaemper RB, Bartyzel P. Medicinal chemistry of serotonergic agents, In Serotonin Receptors, SJ Peroutka ed., Wiley-Liss, NY, in press.
  • 2. Glennon RA, Raghupathi R. Serotonin receptor ligands. Current CNS Patents 1990; 1: 323-343.
  • 3. Pierson ME, Lyon RA, Titeler M, Kowalski P, Glennon RA. Design and synthesis of propranolol analogues as serotonergic agents. J Med Chem 1989; 32: 859-863.
  • 4. Glennon RA, Naiman NA, Lyon RA, Titeler M. Arylpiperazine derivatives as high-afflnity 5-HT1A serotonin ligands. J Med Chem 1988; 31: 1968-1971.
  • 5. Glennon RA, Naiman NA, Pierson ME, Titeler M, Lyon RA, Herndon JL, Misenheimer B. Stimulus properties of arylpiperazines: NAN-190, a potential 5-HT1A serotonin antagonist. Drug Dev Res 1989: 16: 335-343.
  • 6. Arbuckle JL, Canan CM, Barrett JE. Antagonism of the discriminative stimulus effects of 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH DPAT) by the putative serotonin 1A antagonist l-(2-meth-oxyphenyl)-4-[4-(2-phthalimido)butyl]piperazine (NAN-190). Soc Neurosci Abstr 1989; 15: 223.
  • 7. Przegalinski E, Ismaiel AM, Chojnacka-Wójcik E, Budziszewska B, Tatarczynska E, Blaszczynska E. The behavioral, but not the hypothermic or corticosterone, response to 8-hydroxy-2- (di-n-propylamino)teralin is antagonized by NAN-190 in the rat. Neuropharmacology 1990; 6: 521-526.
  • 8. Rydelek-Fitzgerald L, Teitler M, Fletcher PW, Ismaiel AM, Glennon RA. NAN-190: Agonist and antagonist interactions with brain 5-HT1A receptors. Br in Res, in press.
  • 9. Hjorth S, Sharp T. Mixed agonist/antagonist properties of NAN-190 at 5-HT1A receptors: Behavioural and in vivo brain microdialysis studied. Life Sci 1990; 46: 955-963.
  • 10. Raghupathi R, Rydelek-Fitzgerald L, Teitler M, Glennon RA. Development of selective/potent 5-HT1A antagonists. Soc Neurosci Abstr 1990; 16: 1036.
  • 11. Glennon RA, Seggel MR. Interaction of phenylisopropylamines with central 5-HT2 receptors: A QSAR analysis. In: Probing Bioactive Mechanisms, PS Magee, DR Henry, JH Block, eds ACS Press, Washington DC, 1989 p. 264-280.
  • 12. Seggel MR, Yousif MY, Lyon RA, Titeler M, Roth BL, Suba EA, Glennon RA. A structure- affinity study of the binding of 4-substituted analogues of l-(2,5-dimethoxyphenyl)-2-amino- propane at 5-HT2 serotonin receptors. J Med Chem 1990; 33: 1032-1036.
  • 13. Glennon RA, Chaurasia C, Titeler M. Binding of indolylalkylamines at 5-HT2 serotonin receptors: Examination of a hydrophobic binding region. J Med Chem 1990; 33: 2777-2794.
  • 14. Glennon RA, Peroutka SJ, Dukat M. Binding characteristics of a quaternary salt of serotonin: 5-HTQ. Abstracts of the Second IUPHAR Satellite Meeting on Serotonin, Basel, Switzerland; July, 1990. p. 42.
  • 15. Glennon RA. Do classical hallucinogens act as 5-HT2 agonists or antagonists? Presented at the Maui Serotonin Symposium, Maui, Hawaii; December, 1989.
  • 16. Darmani NA, Martin BR, Pandey U, Glennon RA. Do functional relationships exist between 5-HT1A and 5-HT2 receptors? Pharmacol Biochem Behav 1990; 36: 901-906.
  • 17. Arnt J, Hyttel J. Importance of 5-HT1A and 5-HT2 receptors in the expression of forepaw treading and head twitches. Soc Neurosci Abstr 1989; 15: 22.
  • 18. Yocca FD, Wright RN, Margraf RR, Eison AS. 8-OH DPAT and buspirone analogs inhibit the ketanserin sensitive quipazine-induced head shake response in rats. Pharmacol Biochem Behav 1990; 35: 251-254.
  • 19. Darmani NA, Martin BR, Pandey U, Glennon RA. Pharmacological characterization of the earscratch response in mice as a behavioral model for selective 5-HT2-receptor agonists and evidence for 5-HT1B and 5-HT2 receptor interactions. Pharmacol Biochem Behav 1990; 37: 95-99.
  • 20. Glennon RA. Discriminative stimulus properties of hallucinogens and related designer drugs. Psychopharmacology 1990; 101: S68.
  • 21. Hilver SE, Bjork L, Li YL, Svensson B, Ross S., Anden NE, Hackseil U. S-5-Fluoro-8-hydroxy-2-(dipropylamino) tetralin: A putative 5-HTlA-receptor antagonist. J. Med Chem 1990 ; 33: 1541-1544.
  • 22. Macor JE, Burkhart CA, Heym JH, Ives JL, Lebel LA, Newman ME, Nielsen JA, Ryan K„ Schulz DW, Torgersen LK, Koe BK. 3-(l,2,5,6-Tetrahydropyrid-4-yl)pyrrolo[3,2-b]pyrid-5-one: A potent and selective serotonin (5-HT1B) agonist and rotationally restricted phenolic analogues of 5-methoxy-3-(l,2,5,6-tetrahydropyrid-4-yl)indole. J Med Chem 1990; 33: 2087- 2093.
  • 23. Kilpatrick GJ, Butler A, Burridge J, Oxford, AW. l-(m-Chlorophenyl)-biguanide, a potent high affinity 5-HT3 receptor agonist. Eur J Pharmacol 1990; 182: 193-197.

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Bibliografia

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