Development of trans-2-[1H-imidazol-4-yl] cyclopropane derivatives as new high-affinity histamine H3 receptor ligands

Journal of Pharmacology and Experimental Therapeutics

Volumn 289, Issue 2, 1999, Pages 1160-1168

  Tedford, Clark E ^a   Phillips, James G ^a   Gregory, Rosilyn ^a   Pawlowski, Gary P ^a   Fadnis, Leena ^a   Khan, M Amin ^a   Ali, Syed M ^a   Handley, Michael K ^a   Yates, Stephen L ^a  

^a GUILFORD PHARMACEUTICALS INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 (1H IMIDAZOL 4 YL)CYCLOPROPANE DERIVATIVE; 4 (2 (5,5 DIMETHYLHEX 1 YNYL)CYCLOPROPYL)IMIDAZOLE; 5 CYCLOHEXYL 1 (4 IMIDAZOL 4 YLPIPERIDYL)PENTAN 1 ONE; CLOBENPROPIT; CYCLOPROPANE DERIVATIVE; HISTAMINE H3 RECEPTOR; IODOPROXYPHAN; THIOPERAMIDE; UNCLASSIFIED DRUG; VERONGAMINE;

ANIMAL CELL; ANIMAL TISSUE; AREA UNDER THE CURVE; CONFERENCE PAPER; DRUG POTENCY; DRUG SELECTIVITY; GENETIC HETEROGENEITY; HISTAMINE RELEASE; LIGAND BINDING; MALE; MOLECULAR INTERACTION; NONHUMAN; PRIORITY JOURNAL; RAT; RECEPTOR AFFINITY; RECEPTOR OCCUPANCY; STRUCTURE ACTIVITY RELATION;

ANIMALS; BINDING, COMPETITIVE; BUFFERS; CEREBRAL CORTEX; HISTAMINE ANTAGONISTS; HUMANS; IMIDAZOLES; LIGANDS; MALE; RADIOLIGAND ASSAY; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, HISTAMINE H3; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 0032954385     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Conference Paper

References (27)

1. 3 receptor antagonists. J Med Chem 42:903-909.
2. 3 receptor antagonists derived form the marine natural product verongamine. Biorg Med Chem Lett 8:1133-1138.
3. 3-receptors. Nature (Lond) 327:117-123.
4. 3 receptor subtypes. Br J Pharmacol 107:919-923.
5. 3-receptors in rat cerebral cortical membranes. Br J Pharmacol 114:357-362.
6. 35S]GTPγ[S] binding to pertussis toxin. Eur J Pharmacol 296:223-225.
7. Costa T, Lang J, Glees C and Herz A (1990) Spontaneous association between opioid receptors and GTP-binding regulatory proteins in native membranes: Specific regulation by antagonists and sodium ions. Mol Pharmacol 37:383-394.
8. Costa T, Ogino Y, Munson PJ, Onaran HO and Rodbard D (1992) Drug efficacy at guanine nucleotide-binding regulatory protein-linked receptors: Thermodynamic interpretation of negative antagonism and of receptor activity in the absence of ligand. Mol Pharmacol 41:549-560.
9. 3 receptor antagonists utilizing high performance liquid chromatography and dabsyl derivatization. J Chromatogr B 716: 239-249.
10. Lefkowitz RJ, Cotecchia S, Samama P and Costa T (1993) Constitutive activity of receptors coupled to guanine nucleotide regulatory proteins. Trends Pharmacol Sci 14:303-307.
11. 3 receptor heterogeneity? J Pharmacol Exp Ther 276:1009-1015.
12. 3-antagonist from the marine sponge Verongula gigantea. J Nat Prod 57:175-177.
13. Milligan G and Bond RA (1997) Inverse agonism and the regulation of receptor number. Trends Pharmacol Sci 18:468-474.
14. Milligan G, Bond RA and Melanie L (1995) Inverse agonism: Pharmacological curiosity or potential therapeutic strategy? Trends Pharmacol Sci 16:10-13.
15. 2-adrenergic receptor. J Biol Chem 268:4625-4636.
16. 3 receptor heterogeneity. Naunyn-Schmiedeberg's Arch Pharmacol 353:482-488.
17. 3 receptor heterogeneity. Naunyn-Schmiedeberg's Arch Pharmacol 350:375-379.
18. 2 receptors. Proc Natl Acad Sci USA 93:6802-6802.
19. 3-receptor antagonists. Drugs Future 21:507-520.
20. 3 receptors by thioperamide and (R)-a-methyhistamine measured using histamine turnover and an ex vivo labeling technique. Biochem Pharmacol 44:1261-1267.
21. 3 receptor antagonists. Eur J Pharmacol 351:307-311.
22. 3 antagonist; in vitro and in vivo studies. J Pharmacol Exp Ther 275:598-604.
23. Topliss JG (1972) Utilization of operational schemes for analog synthesis in drug design. J Med Chem 15:1006-1011.
24. 3-receptor. Eur J Med Chem 27:511-518.
25. White DW, Wang Y, Chua SC Jr, Morgenstern JP, Leibel RL, Baumann H and Tartaglia LA (1997) Constitutive and impaired signaling of leptin receptors containing the Gln-Pro extracellular domain fatty mutation. Proc Natl Acad Sci 94:10657-10662.
26. 3-histamine receptor subtypes. Mol Pharmacol 38:610-613.
27. 3 receptor ligands. J Pharmacol Exp Ther 289:1151-1159.