Most Axon Ligands™ in this category of compounds are labeled antipsychotic (typical, or atypical), since many of the common drugs to treat this class of mental disorders show affinity for both dopaminergic and serotonergic receptors (among several others). The first generation of antipsychotics (typical), developed in the 1950’s consisted of mainly phenothiazines (chlorpromazine)[1], and butyrophenones (haloperidol)[2]. Though still considered benchmark antipsychotics[3], they are known for there unwanted side effects such as dry mouth, extra pyramidal side effects, and tardive dyskinesia[4]. The atypical antipshychotics, or second generation antipsychotics, are less likely to cause the afore mentioned side effects, and improve the quality of live compared to the typical antipsychotics. However, this class of drugs is also far from free of side effects[5]. Among them, many Clozapine (Axon 1146) analogues, Aripiprazole (Axon 1143), and Ziprazidone (Axon 1446).
Based on a phylogenetic analysis, the family of serotonin (5-HT) receptors should be separated into two different classes among the subgroup of biogenic amine receptors of the rhodopsin-like family of GPCRs. The GPCR-A17 class includes all 5-HT2 and 5-HT6 receptors, while 5-HT1, 5-HT4 5HT-5 and 5HT7 receptors form an individual class: GPCR-A19[6].

5-HT receptor subtypes listed: 5-HT1A5-HT1B5-HT1D5-HT1F5-HT2 ,5-HT2A5-HT2C5-HT45-HT5A5-HT65-HT7

[1] Recherches sur les diméthylaminopropyl-N phénothiazines substituées. Charpentier P, Gailliot P, Jacob R, et al. Comptes rendus de l’Académie des sciences (Paris), 1952, 235, 59–60.
[2] Haloperidol: fifteen years of clinical experience. Ayd FJ. Diseases of the Nervous System 1972, 33, 459–69.
[3] Haloperidol versus chlorpromazine for treatment of schizophrenia. C. Leucht, M. Kitzmantel, L. Chua, J. Kane, and S. Leucht. Schizophr Bull 2008, 34, 813-815.
[4] Antipsychotics - the future of schizophrenia treatment. G. Beaumont. Curr Med Res Opin. 2000,16, 37-42.
[5] Side effects of atypical antipsychotics: a brief overview. A. Üçok and W. Gaebel. World Psychiatry. 2008, 7, 58–62.
[6] P. Joost, A. Methner. Phylogenetic analysis of 277 human G-protein-coupled receptors as a tool for the prediction of orphan receptor ligands. Gen. Biol. 2002, 3, 0063.

28 Item(s)

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Axon ID Name Description From price
1107 (+)-MDL 105725 5-HT2A antagonist €130.00
1108 (-)-MDL 105725 5-HT2A antagonist Inquire
1106 (±)-MDL 105725 5-HT2A antagonist €160.00
2811 25CN-NBOH hydrochloride Selective brain penetrant 5-HT2A receptor agonist €150.00
1143 Aripiprazole Atypical antipsychotic €75.00
1503 Asenapine maleate Atypical antipsychotic €70.00
2335 Brexpiprazole dihydrochloride Drug candidate with high affinity for 5-HT1A, 5-HT2A, D2L, α1B, and α2C-adrenergic receptors €135.00
1146 Clozapine Atypical antipsychotic €50.00
3511 Cyproheptadine hydrochloride 5-HT2A and H1 antagonist €50.00
1439 Eplivanserin 5-HT2A antagonist/inverse agonist €80.00
1499 Flibanserin 5-HT1A agonist and 5-HT2A antagonist €95.00
2851 GMC 1-161 Clozapine analog with 5-HT2A, M1 and D2 affinity, devoid of D1 affinities €135.00
1152 GMC 1-165 Clozapine analog with 5-HT2A and M1 affinity, devoid of D1/D2 affinities €135.00
1148 GMC 1-169 Atypical antipsychotic €150.00
1150 GMC 2-83 Atypical antipsychotic €150.00
1149 GMC 61-39 Atypical antipsychotic Inquire
3925 IHCH-7079 5-HT2A receptor arrestin-biased agonist €150.00
1493 Iloperidone Atypical antipsychotic €85.00
1147 Isoclozapine Typical antipsychotic €135.00
1450 Ketanserin 5-HT2A antagonist €55.00
1105 MDL 100009 5-HT2A antagonist €125.00
1103 MDL 100151 5-HT2A antagonist €110.00
1104 MDL 100907 5-HT2A antagonist €110.00
1102 Nefazodone hydrochloride Antidepressant; 5-HT2A antagonist €85.00
1247 PNU 22394 hydrochloride Potent 5-HT ligand with full agonistic properties for 5-HT2C €90.00
3859 Roluperidone Sigma-2 and 5-HT2A receptor antagonist €120.00
1144 Thio-aripiprazole Atypical antipsychotic €140.00
1446 Ziprasidone hydrochloride Atypical antipsychotic €50.00

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