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. 2015 Aug 7;6:162. doi: 10.3389/fphar.2015.00162

Table 2.

Selected overview on available 5-HT1A receptor antagonists.

Function Compound Receptor specificity MW Solvent BBB penetr. Behavior Reference
Partial BMY-7378 5-HT1A >> α1 >> α2 (partial agonist function) >> 5-HT7 >> 5-HT 1D 385.9 W + A, L Greuel and Glaser (1992), Grasby et al. (1992)
Partial LY-426965 HT1A >> 5-HT1B (partial agonist function) 471.1 W n.a. A Rasmussen et al. (2000); http://sis.nlm.nih.gov/
MC18 fumarate 5-HT1A >> n.a 515.7 W n.a. L Pittalà et al. (2015)
MP3022

NAD-299 (Robalzotan		 5-HT1A >> α1 >> 5-HT2A, α2, β, D1 and D2
5-HT1A >> α1,α2, β		 351.5 354.9 n.a.

W		 n.a.

+		 n.a.

A, L		 Filip and Przegaliñski (1996)
Johansson et al. (1997), Madjid et al. (2006); http://chem.sis.nlm.nih.gov/
Partial NAN-190 HT1A >> α1 (partial agonist function reported) >> 5-HTR, D 393.5 W n.a. A, L Raghupathi et al. (1991), Greuel and Glaser (1992)
p-MPPI 5-HT1A >> α1 542.4 W + A Kung et al. (1994), Allen et al. (1997); http://pubchem.ncbi.nlm.nih.gov/
p-MPPF 5-HT1A >> α1 507.4 n.a. + n.a. Kung et al. (1996), Passchier et al. (2000); http://pubchem.ncbi.nlm.nih.gov/
SB-649915 n.a., combined function as 5-HT1A/B autoreceptor antagonist and SSRI n.a. MC n.a. A Starr et al. (2007)
Spiperone 5-HT1A >> 5-HT2A/c >> D2 antagonist and αlb antagonist n.a. MC n.a. A Starr et al. (2007)
SRA-333 (Lecozotan) 5-HT1A >> α1 >> D2 >> D3 >> D4 (α and D agonist) n.a. W n.a. A, L Schechter et al. (2005)
(S)-UH-301 5-HT1A >> D2, D3 (agonist) 301.8 W Yes A, L Moreau et al. (1992), Jackson et al. (1994)
VP-08/34 fumarate 5-HT1A >> n.a 513.6 W Yes L Pittalà et al. (2015)
WAY-100635 5-HT1A >> α1 >> D2 >> D3 >> D4 538.6 W Yes A, L Fletcher et al. (1996), Pike et al. (1996)
WAY-405 5-HT1A >> α n.a. MC Yes A, L Minabe et al. (2003), Villalobos-Molina et al. (2005)
WAY-101405 5-HT1A >> n.a n.a. W Yes L Hirst et al. (2008)

A, anxiety; BBB, blood–brain barrier; D: FST, forced swim test; L, learning and memory tests; MC, methylcellulose; n.a., not available; penetr., penetrance; PPI, pre-pulse inhibition; S*, 2-hydroxypropyl-β-cyclodextrin; W, soluble in water and/or saline.