Molecular Design of Novel Ligands for 5-HT_1A Receptors

References

• Rapport M. M. Serum Vasoconstrictor (serotonin), V. The Presence of Creatinine in the Complex: A Proposed Study of the Vasoconstrictor Principle. J. Biol. Chem. 1949; 180: 961–969
   PubMed Web of Science ®Google Scholar
• Gaddum J. H., Picarelli Z. P. Two Kinds of Tryptamine Receptor. Br J. Pharmac. 1957; 12: 323–328
   PubMed Web of Science ®Google Scholar
• Peroutka S. J., Snyder S. H. Two Distinct Serotonin Receptors: Regional Variations in Receptor Binding in Mammalian Brain. Brain Res. 1981; 208: 339–347
   PubMed Web of Science ®Google Scholar
• Fargin A., Raymond J. R., Lohse M. J., Kobilka B. K., Caron M. C., Lefkowitz R. J. The Genomic Clone G-21 which Resembles a β-Adrenergic Receptor Sequence Encodes the 5-HT1A Receptor. Nature 1988; 335: 358–360
   PubMed Web of Science ®Google Scholar
• Julius D., MacDermott A. B., Axel R., Jessell T. M. Molecular Characterization of a Functional cDNA Encoding the Serotonin 1C Receptor. Science 1988; 24: 558–564
   Google Scholar
• Peroutka S. J. 5-Hydroxytryptamine Receptor Subtypes: Molecular, Biochemical and Physiological Characterization. Trends in Neurosci. (TINS) 1988; 11: 486–500
   Google Scholar
• Mylecharane E. W. The Classification of 5-Hydroxytryptamine Receptors. Clin. Exper. Pharmacol. Physiol. 1989; 15: 517–522
   Google Scholar
• Clarke D. E., Craig D. A., Fozard J. R. The 5-HT4 Receptor: Naughty, but Nice. Trends in Pharmacol. Sci. (TIPS) 1989; 10: 385–386
   PubMed Web of Science ®Google Scholar
• Nava-Felix P., Hong E. Nature of the Central Serotonin Receptors Mediating Hypotension, J. Cardio. Pharmacol. 1979; 1: 461–466
   Google Scholar
• Hjorth S., Carlsson A., Lindberg P., Sanchez D., Wikstrom H., Arvidsson L.-E., Hacksell U., Nilsson J. L.G. 8-Hydroxy-2-(Di-n-Propylamino) Tetralin, 8-OH-DPAT, a Potent and Selective Simplified Ergot Congener with Central 5-HT-Receptor Stimulating Activity. J. Neur. Trans. 1982; 55: 169–199
   Google Scholar
• Gradin K., Pettersson A., Hjorth S., Hedner T., Arvidsson L. E., Persson P. Cardiovascular effects in the Sprague-Dawley rat of 8-Hydroxy-2-(Di-n-Propylamino) Tetralin a Selective 5-Hydroxytryptamine Receptor Agonist. J. Pharm. Pharmacol. 1985; 37: 263–265
   PubMedGoogle Scholar
• Dabire H., Cherqui C., Fournier B., Schmitt H. Comparison of Effects of some 5-HT1 Agonists on Blood Pressure and Heart Rate of Normotensive Anaesthetized Rats. Eur. J. Pharmacol. 1987; 140: 259–266
   PubMed Web of Science ®Google Scholar
• Martin G. E., Lis E. V., Jr. Hypotensive Action of 8-Hydroxy-2-(Di-n-Propylamino) Tetralin (8-OH-DPAT) in Spontaneously Hypertensive Rats. Arch. Internat, de Pharmacodynamie Ther. 1985; 273: 251–261
   PubMedGoogle Scholar
• Fozard J. R., Mir A. K., Middlemiss D. N. Cardiovascular Response to 8-Hydroxy-2-(Di-n-Propylamino) Tetralin (8-OH-DPAT) in the Rat: Site of Action and Pharmacological Analysis. J. Cardio. Pharmacol. 1987; 9: 328–347
   PubMed Web of Science ®Google Scholar
• Di Francesco G. F., Petty M. A., Fozard J. R. Antihypertensive Effects of 8-Hydroxy-2-(Di-n-Propylamino) Tetralin (8-OH-DPAT) in Conscious Dogs. Eur. J. Pharmacol. 1988; 147: 287–290
   PubMedGoogle Scholar
• Doods H. N., Kalkman H. O. A., De Jonge M., Thoolen J. M.C., Wilffert B. P.B., Timmermans M. W.M., Van Zwieten P. A. Differential Selectivities of RU 24969 and 8-OH-DPAT for the Purported 5-HT and 5-HT1B Binding Sites. Correlation Between 5-HT1A Affinity and Hypotensive Activity. Eur. J. Pharmacol. 1985; 112: 363–370
   PubMedGoogle Scholar
• Gillis R. A., Hill K. J., Kirby J. S., Quest J. A., Hamosh P., Norman W. P., Kellar K. J. Effect of Activation of Central Nervous System Serotonin 1A Receptors on Cardiorespiratory Function. J. Pharmacol. Exp. Ther. 1989; 248: 851–856
   PubMedGoogle Scholar
• Doods H. N., Boddeke H. W.G.M., Kalkman H. O., Hoyer D., Mathy M.-J., Van Zwieten P. A. Central 5-HT Receptors and the Mechanism of the Central Hypotensive Effect of (+)8-OH-DPAT, DP-5-CT, R28935, and Urapidil. J. Card. Pharmacol. 1988; 11: 432–437
   PubMedGoogle Scholar
• Sanders K. H., Beller K.-D., Bischler P., Kolassa N. Interaction of Urapidil with Brain Serotonin-1A Receptors Increases the Blood Pressure Reduction due to Peripheral Alpha-adreoceptor Inhibition. J. Hypertens. 1988; 6(Suppl. 2)S65–S68
   Google Scholar
• Wouters W., Tulp M. M. Th., Sevan P. Flesinoxan Lowers Blood Pressure and Heart Rate in Cats via 5-HT Receptors. Eur. J. Pharmacol. 1988; 149: 213–223
   PubMedGoogle Scholar
• Schoeffter P., Hoyer D. Centrally Acting Hypotensive Agents with Affinity for 5-HT1A Binding Sites Inhibit Forskolin-stimulated Adenylate Cyclase Activity in Calf Hippocampus. Br. J. Pharmacol. 1988; 95: 975–985
   PubMedGoogle Scholar
• Hof R. P., Fozard J. R. 8-OH-DPAT, Flesinoxan and Guanfacine: Systemic and Regional Haemodynamic Effects of Centrally Acting Antihypertensive Agents in Anaesthetized Rabbits. Br. J. Pharmacol. 1989; 96: 864–871
   PubMedGoogle Scholar
• Ramage A. G., Wouters W., Bevan P. Evidence that the Novel Antihypertensive Agent, Flesinoxan, causes Differential Sympathoinhibition and also Increases Vagal Tone by a Central Action. Eur. J. Pharmacol. 1988; 151: 373–379
   PubMedGoogle Scholar
• Arvidsson L.-E, Hacksell U., Nilsson J. L.G., Hjorth S., Carlsson A., Lindberg P., Sanchez D., Wikstrom H. 8-Hydroxy-2-(di-n-propylamine) tetralin, a New Centrally acting 5-Hydroxy-tryptamine Receptor Agonists. J. Med. Chem. 1981; 24: 921–923
   PubMed Web of Science ®Google Scholar
• Arvidsson L.-E, Hacksell U., Johansson A. M., Nilsson J. L.G., Lindberg P., Sanchez D., Wikstrom H., Svensson K., Hjorth S., Carlsson A. 8-Hydroxy-2-(alkylaminc) tetralins and related Compounds as central 5-Hydroxytryptamine Receptor Agonists. J. Med. Chem. 1984; 27: 45–51
   PubMedGoogle Scholar
• Arvidsson L-E., Karlen A., Norinder U., Kenne L., Sundell S., Hacksell U. Structural Factors of Importance for 5-Hydroxytryptaminergic Activity. Conformational Preferences and Electrostatic Potentials of 8-Hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) and some Related Agents. J. Med. Chem. 1988; 31: 212–221
   PubMedGoogle Scholar
• Pedigo N. W., Yamamura H. T., Nelson D. L. Discrimination of Multiple [3H]5-Hydroxytryptamine Binding Sites by the Neuroleptic Spiperone in Rat Brain. J. Neurochem. 1981; 36: 220–226
   PubMed Web of Science ®Google Scholar
• Blurton P. A., Wood M. D. Identification of Multiple Binding Sites for [3H]5-Hydroxytryptamine in the Rat CNS. J. Neurochem. 1986; 46: 1392–1398
   PubMed Web of Science ®Google Scholar
• Stanisic D., Hancock A. A., Meyer M., DeBernardis J. F. Stereo-selective Discrimination of Serotoninergic 5HT-1A and 5HT-1B Binding Sites using the Enantiomers of Spiroxatrine and WB-4101. FASEB J. 1988; 2: A-1399
   Google Scholar
• Nelson D. L., Taylor E. W. Spiroxatrine: A Selective Serotonin 1A Receptor Antagonist. Eur. J. Pharmacol. 1986; 124: 207–208
   PubMedGoogle Scholar
• Hoyer Pazos D. A., Probst A., Palacios J. M. Serotonin Receptors in the Human Brain. I. Characterization and autoradiographic localization of 5-HT1A Recognition Sites. Apparent absence of 5-HT1B recognition sites. Brain Res. 1986; 376: 85–96
   PubMed Web of Science ®Google Scholar
• Leysen J. E., Niemegeers C. J.E., Van Neuten J. M., Laduron P. M. [3H]Ketanserin (R 41468), a Selective H-Ligand for Serotonin Receptor Binding Sites: Binding Properties, Brain Distribution, and Functional Role. Mol. Pharmacol. 1982; 21: 301–314
   PubMed Web of Science ®Google Scholar
• Hancock A. A., Kyncl J. J., Martin Y. C., DeBernardis J. F. Differentiation of Alpha-Adrenergic Receptors Using Pharmacological Evaluation and Molecular Modeling of Selective Adrenergic Agents. J. Receptor Res. 1988; 8: 23–46
   PubMed Web of Science ®Google Scholar
• Hancock A. A., DeLean A. L., Lefkowitz R. J. Quantitative Resolution of beta-adrenergic Receptor Subtypes by Selective Ligand Binding: Application of a Computer Model-fitting Technique. Mol. Pharmacol. 1979; 16: 1–9
   PubMed Web of Science ®Google Scholar
• Hancock A. A., Kyncl J. J., Martin Y. C., DeBernardis J. F. Differentiation of Alpha-Adrenergic Receptors Using Pharmacological Evaluation and Molecular Modeling of Selective Adrenergic Agents. J. Receptor Res. 1988; 8: 23–46
   PubMed Web of Science ®Google Scholar
• Doxey J. C., Smith C. F.C., Walker J. M. Selectivity of BLocking Agents for Pre-and Postsynaptic alpha-adrenoceptors. Br. J. Pharmacol. 1977; 60: 91–96
   PubMed Web of Science ®Google Scholar
• Goodwin G. M., De Souza R. J., Green A. R. The Pharmacology of the Hypothermic Response in mice to 8-Hydroxy-2-(Di-n-Propyl-amino)-tetralin (8-OH-DPAT). Neuropharmacol. 1985; 24: 1187–1194
   PubMedGoogle Scholar
• Meyer M. D., Sippy K. B., Hancock A. A., Stanisic D. S., Lee J. Y., Buckner S., DeBernardis J. F. Synthesis and Structure Activity Studies on a Series of Tricyclic Tertiary Amines with High Affinity and Selectivity for the 5-HT1A Subtypes of the Serotonin Receptor. Abstracts of the 198th American Chemical Society Meeting, 197: MEDI. 1990, in press
   Google Scholar
• Yocca F. D., Hyslop D. K., Smith D. W., Maayani S. BMY-7378, A buspirone analog with high-affinity, selectivity, and low intrinsic activity at the 5-HT receptor in rat and guinea pig hippocampal membranes. Eur. J. Pharmacol. 1987; 137: 293–294
   PubMed Web of Science ®Google Scholar
• Rowan M. J., Anwyl R. Neurophysiological effects of buspirone and isapirone in the hippocampes: comparison with 5-hydroxytryptamine. Eur. J. Pharmacol. 1987; 132: 93–96
   Google Scholar
• Dunwiddie T., Mueller A., Basile A. The use of biain slices in central nervous system pharmacology. Fed. Proc 1983; 42: 2891–2898
   PubMedGoogle Scholar