5-HT2C
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-HT1A, 5-HT1B, 5-HT1D, 5-HT1F, 5-HT2 ,5-HT2A, 5-HT2C, 5-HT4, 5-HT5A, 5-HT6, 5-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.
| Axon ID | Name | Description | From price | |
|---|---|---|---|---|
| 1492 | Agomelatine | Melatonin agonist; 5-HT2C antagonist | €75.00 | |
| 1503 | Asenapine maleate | Atypical antipsychotic | €70.00 | |
| 1146 | Clozapine | Atypical antipsychotic | €50.00 | |
| 1142 | Eltoprazine hydrochloride | 5-HT1A and 5-HT1B agonist | €82.00 | |
| 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 | |
| 1493 | Iloperidone | Atypical antipsychotic | €85.00 | |
| 1147 | Isoclozapine | Typical antipsychotic | €135.00 | |
| 1138 | Mirtazapine | 5-HT antidepressant | €65.00 | |
| 1214 | MK 212 hydrochloride | 5-HT2C agonist | €75.00 | |
| 1298 | Olanzapine | Atypical antipsychotic | €75.00 | |
| 1247 | PNU 22394 hydrochloride | Potent 5-HT ligand with full agonistic properties for 5-HT2C | €90.00 | |
| 1118 | RO 60-0175 | 5-HT2C agonist | €140.00 | |
| 4092 | SB 242084 | Selective 5-HT2C receptor antagonist | €110.00 | |
| 1745 | SB 242084 hydrochloride | Selective 5-HT2C receptor antagonist | €110.00 | |
| 2889 | VA012 | Positive allosteric modulator (PAM) of 5-HT2C receptor | €105.00 | |
| 1446 | Ziprasidone hydrochloride | Atypical antipsychotic | €50.00 | |