(±)-1-(2,5-dimethoxy-4-ethylthiophenyl)-2-aminopropane (ALEPH-2), a novel putative anxiolytic agent lacking affinity for benzodiazepine sites and serotonin-1A receptors

Naunyn-Schmiedeberg's Archives of Pharmacology

Volumn 354, Issue 5, 1996, Pages 579-585

  Reyes Parada, Miguel ^a   Scorza, Cecilia ^a   Romero, Veronica ^a   Silveira, Rodolfo ^a   Medina, Jorge H ^b   Andrus, Danice ^c   Nichols, David E ^c   Cassels, Bruce K ^d  

^a INSTITUTO DE INVESTIGACIONES BIOLÓGICAS CLEMENTE ESTABLE   (Uruguay)

^b Facultad de Medicina   (Argentina)

^c PURDUE UNIVERSITY   (United States)

^d UNIVERSITY OF CHILE   (Chile)

Author keywords

ALEPH 2; Anxiolytics; Hypothermia; Phenylisopropylamines; Psychedelics; Rat; Serotonin receptor binding; Serotonin syndrome

Indexed keywords

2 DIPROPYLAMINO 8 HYDROXYTETRALIN; AMIFLAMINE; AMPHETAMINE DERIVATIVE; ANXIOLYTIC AGENT; BENZODIAZEPINE RECEPTOR; BUSPIRONE; CINANSERIN; KETANSERIN; MUSCIMOL; SEROTONIN; SEROTONIN RECEPTOR; 1 (2,5 DIMETHOXY 4 ETHYLTHIOPHENYL) 2 AMINOPROPANE; 1-(2,5-DIMETHOXY-4-ETHYLTHIOPHENYL)-2-AMINOPROPANE; 2,5 DIMETHOXY 4 METHYLAMPHETAMINE; 4 AMINOBUTYRIC ACID A RECEPTOR; DRUG DERIVATIVE; SEROTONIN ANTAGONIST;

ANIMAL EXPERIMENT; ARTICLE; BEHAVIOR; BODY TEMPERATURE; CONTROLLED STUDY; DRUG MECHANISM; DRUG RECEPTOR BINDING; HYPOTHERMIA; INTRAPERITONEAL DRUG ADMINISTRATION; MALE; NONHUMAN; RAT; RODENT; TRANQUILIZING ACTIVITY; ANALYSIS OF VARIANCE; ANIMAL; ANIMAL BEHAVIOR; BINDING SITE; CHEMICALLY INDUCED DISORDER; DOSE RESPONSE; DRUG EFFECT; METABOLISM; MOTOR ACTIVITY; MOUSE; PHYSIOLOGY; RADIOASSAY; WISTAR RAT;

2,5-DIMETHOXY-4-METHYLAMPHETAMINE; ANALYSIS OF VARIANCE; ANIMALS; ANTI-ANXIETY AGENTS; BEHAVIOR, ANIMAL; BINDING SITES; BODY TEMPERATURE; DOSE-RESPONSE RELATIONSHIP, DRUG; HYPOTHERMIA; KETANSERIN; MALE; MICE; MOTOR ACTIVITY; RADIOLIGAND ASSAY; RATS; RATS, WISTAR; RECEPTORS, GABA-A; RECEPTORS, SEROTONIN; SEROTONIN ANTAGONISTS;

EID: 0029658459     PISSN: 00281298     EISSN: None     Source Type: Journal    
DOI: 10.1007/BF00170831     Document Type: Article

References (40)

1. Barrett JE, Vanover KE (1993) 5-HT receptors as targets for the development of novel anxiolytic drugs: models, mechanism and future directions. Psychopharmacology 112:1-12
2. Bedard P, Pycock CJ (1977) "Wet dog shake" behaviour in the rat: a possible quantitative model of central 5-hydroxytryptamine activity. Neuropharmacology 16:663-670
3. 2 receptor down regulation results in anxiolytic effects in the elevated plus-maze test. Drug Dev Res 26:287-297
4. 1C receptor agonist. J Pharmacol Exp Ther 258:891-896
5. 3 antagonists and benzodiazepines: their comparative behavioural pharmacology. Wiley, Chiehesler, England, pp 133-157
6. 2 receptors. Psychopharmacology 93:502-506
7. 1A receptors in anxiety. In: Briley M, File SH (eds) New concepts in anxiety. CRC Press, Boca Raton, FL, pp 94-129
8. Feighner JP, Merideth CH, Hendrickson GA (1982) Double-blind comparison of buspirone and diazepam in outpatients with generalized anxiety disorder. J Clin Psychiatry 43:103-107
9. Gammans RE, Stringfellow JC, Hvizdos AJ, Seidehamel RJ, Cohn JB, Wilcox CS, Fabre LF, Pecknold JC, Smith WT, Rickels K (1992) Use of buspirone in patients with generalized anxiety-disorder and coexisting depressive symptoms. A meta-analysis of eight randomized controlled studies. Neuropsychobiology 25:193-201
10. 2 agonists or antagonists? Neuropsychopharmacology 3:509-517
11. Glennon RA, Lucki I (1988) Behavioral models of serotonin receptor activation. In: Sanders-Bush E (ed) Serotonin. Humana Press, Clifton Park, N.J., pp 253-294
12. 2 involvement in the mechanism of action of hallucinogenic agents. Life Sci 35:2505-2511
13. 2 serotonin receptors: evidence for a lack of selectivity. J Med Chem 35:734-740
14. Green AL, El Hait MAS (1980) p-Methoxyamphetamine, a potent reversible inhibitor of type-A monoamine oxidase in vitro and in vivo. J Pharm Pharmacol 32:262-266
15. 1A receptors. Neuropharmacology 25:1307-1313
16. Handley SL, McBlane JW, Critchley MAE, Njung'e K (1993) Multiple serotonin mechanism in animal models of anxiety: environmental, emotional and cognitive factors. Behav Brain Res 58:203-210
17. Huang X, Marona-Lewicka D, Nichols DE (1992) p-Methylthioamphetamine is a potent new nonneurotoxic serotonin-releasing agent. Eur J Pharmacol 229:31-38
18. 2 receptor in rat frontal cortex. Pharmacol Biochem Behav 35:211-217
19. Kahn RS, Van Praag HM, Wetzler S, Asnis GM, Barr G (1988) Serotonin and anxiety revisited. Biol Psychiatry 23:189-208
20. 1C receptor antagonists have anxiolytic-like actions in the rat social interaction test. Psychopharmacolocy 107:397-402
21. 1C receptor antagonists. Eur J Pharmacol 164:445-454
22. 2C receptor antagonists are anxiolytic in the rat Geller-Seifter model of anxiety. Psychopharmacology 114:90-96
23. Klodzinska A, Chojnacka-Wojcik E (1992) Hyperthermia induced by m-trifluoromethylpiperazine (TFMPP) or m-chlorophenylpiperazine (m-CPP) in heat adapted rats. Psychopharmacology 109:466-472
24. 1C receptors. Neurosci Biobehav Rev 16:95-105
25. 1A autoreceptor response and its evaluation as a model to selectively identify antidepressants. Br J Pharmacol 107:15-21
26. McPherson G (1985) Analysis of radioligand binding experiments: A collection of computer programs for the IBM PC. J Pharmacol Methods 14:213-218
27. Murphy DL, Lesch KP, Aulakh CS, Pigott TA (1991) III. Serotonin-selectivc arylpiperazines with neuroendocrine, behavioral, temperature and cardiovascular effects in humans. Pharmacol Rev 43:572-552
28. 2 receptor-mediated temperature and corticosterone responses. Pharmacol Biochem Behav 33:781-785
29. Nichols DE (1994) Medicinal chemistry and structure-activity relationships. In: Cho AK, Segal DS (eds) Amphetamine and its analogs: psychopharmacology, toxicology and abuse. Academic Press, San Diego, Calif, pp. 3-41
30. Nichols DE, Marona-Lewicka D, Huang X, Johnson MP (1993) Novel serotonergic agents. Drug Des Discov 9:299-312
31. Radja F, Daval G, Hamon M, Vergé D (1992) Pharmacological and physiochemical properties of pre versus postsynaptic 5-hydroxytryptamine 1A receptor binding sites in the rat brain: a quantitative autoradiographic study. J Neurochem 58:1338-1346
32. 2 receptors: implications for treating LSD-induced hallucinogenesis. Psychopharmacology 98:495-499
33. Sanders-Bush E, Breeding M (1991) Choroid plexus epithelial cells in primary culture: a model of 5-HT1C receptor activation by hallucinogenic drugs. Psychopharmacology 105:340-346
34. Scorza MC, Reyes-Parada M, Silveira R, Viola H, Medina JH, Viana MB, Zangrossi Jr. H, Graeff FG (1996). Behavioral effects of the putative anxiolytic (±)-1-(2,5-dimethoxy-4-ethylthiophenyl)-2-aminopropane(ALEPH-2) in rats and mice. Pharmacol Biochem Behav 54:355-361
35. Shulgin AT, Shulgin A (1991) In: Phenethylamines I Have Known and Loved. Transform Press, Berkeley, Calif., pp 464-465 and 864-865
36. Tomkins DM, Costall B, Kelly ME (1990) Action of ritanserin and DOI on the elevated X-maze. Psychopharmacology 101:S57
37. Tricklehank MD (1985) The behavioural response to 5-HT receptor agonists and subtypes of the central 5-HT receptor. Trends Pharmacol Sci 6:403-407
38. Tricklebank MD, Forler C, Fozard JR (1985) The involvement of subtypes of the 5-HT, receptor and of catecholaminergic systems in the behavioural response to 8-hydroxy-2-(di-n-propylamino)-tetralin in the rat. Eur J Pharmacol 106:271-282
39. Wozniak KM, Aulakh CS, Hill JL, Murphy DL (1989) Hyperthermia induced by m-CPP in the rat and its modification by antidepressant treatments. Psychopharmacology 97:269-274
40. 2 receptors in the wet-dog shake behaviour induced by 5-hydroxytryptophan in the rat. Neuropharmacology 22:801-804