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123Glennon RA (1992). "Concepts for the design of 5-HT 1A serotonin agonists and antagonists". Drug Development Research. 26 (3): 251–274. doi:10.1002/ddr.430260306. ISSN0272-4391. Fig. 1. Structures of some indolealkylamines: 5-HT 5-CAT (2), RU 24969 (3), (+)LSD (4), RU 28306 (5), BAY R 1531 (6), and LY 178210 (7). [...] Partial ergolines have also been examined [Flaugh et al., 1988]. For example, RU 28306 (5) binds at 5-HT1, sites with relatively low affinity (Ki = 329 nM) [Taylor et al., 1987]; however, the corresponding N,N-dipropyl-6-substituted analogs BAY R 1531 (6) [Glaser et al., 1987] and LY 178210 (7) [Slaughter et al., 1990] bind with significantly higher affinity (Ki <1 nM). These latter two agents, as with O-methyl DiPS [Glennon et al., 1988a] and N,N-dipropyl-5-carboxamidotryptamine [Hibert et al., 1987], possess 5-HT1, agonist activity. The hydroxy analog of compound 6 is apparently a full agonist [Seiler et al., 1990] whereas LY 178210 (7) acts as a partial agonist in an adenylate cyclase assay [Slaughter et al., 1990].
123Audia JE, Cohen ML (1991). "Chapter 11. Serotonin Modulators and Cardiovascular/Gastrointestinal Diseases". Annual Reports in Medicinal Chemistry. Vol.26. Elsevier. pp.103–112. doi:10.1016/s0065-7743(08)61198-7. ISBN978-0-12-040526-8. Ergolines and Partial Ergolines - Although primarily investigated as 5-HT2 receptor ligands, several ergolines, including lisuride and lysergic acid diethylamide (LSD), show high affinity for 5-HT1A receptors, although they lack selectivity (47). Some partial ergolines, including LY 178210 (8) and LY 197206 (9), show surprising selectivity as 5-HT1A agonists relative to related ergolines (65). This specificity, however, can be more readily rationalized by recognizing the similarities to the 5-HT1A-selective aminotetralins [...] From an SAR perspective, a partial ergoline such as LY 178210 (Q) does not retain this high affinity for the 5-HT1C receptor (65). [...] Miscellaneous Structures - Many ergolines, particularly metergoline and methysergide have high affinity for the 5-HT1D receptor, while other ergolines such as mesulergine and the partial ergoline LY 178210 (9) lack significant affinity at this receptor subtype (65).
12Nelson DL (December 1991). "Structure-activity relationships at 5-HT1A receptors: binding profiles and intrinsic activity". Pharmacology, Biochemistry, and Behavior. 40 (4): 1041–1051. doi:10.1016/0091-3057(91)90124-k. PMID1816558. Table 3 Effect on 5-HT1A Affinity by Substitutions at the C6 Position of a Series of Tricyclic Partial Ergolines [...]
12Perregaard J, Sánchez C, Arnt J (1993). "Overview: Recent Developments in Anxiolytics". Current Opinion on Therapeutic Patents. 3 (1): 101–128. doi:10.1517/13543776.3.1.101. ISSN0962-2594. Many of the Lilly compounds (25) were shown to have nanomolar affinity for 5-HT1D, as well as for 5-HT1A, receptors. An exception is the clinical development candidate LY 178210, which has 500-fold less affinity for 5-HT1D receptors than for 5-HT1A receptors [88].
↑Lucot JB, Brame RE, Garrett TL, Pfadenhauer EH, Kumar A, Fick DB, etal. (August 2014). "The broad-spectrum antiemetic effects ETI-385 result from stimulation of 5-HT1A and 5-HT1D receptors". Exp Brain Res. 232 (8): 2699–2707. doi:10.1007/s00221-014-4004-z. PMID24913143. Another hindrance to the clinical evaluation of this mechanism is that both flesinoxan (van Vliet et al. 1996) and LY22879 (pers. com.) induced anxiety in humans.
