D4
Dopamine receptors (GPCR-A17) are widespread in the body of vertebrates, playing major roles in processes of the central nervous system, as well as in the periphery. In the CNS, dopaminergic neurons are critically involved in voluntary movement, memory, learning, sleep, attention, feeding, and rewarding, Well known examples of disorders as a result of malfunction of the central dopaminergic system are Parkinson’s disease (loss of striatal dopaminergic innervations in the brain), schizophrenia, depression, ADHD, and addiction (among many others). In the periphery, dopamine plays important physiological roles in the regulation of olfaction, retinal processes, hormonal regulation, cardiovascular functions, sympathetic regulation, immune system, renal functions, and more[1]. Five major classes (D1-D5) have been identified thus far, which can be grouped into two sub classes. The group of D1-like receptors (members D1 and D5; all stimulating the second messenger system adenylate cyclase), and the group of D2-like receptors (members D2, D3 and D4; all inhibiting adenylate cyclase). As widespread and abundant as dopaminergic neurons are in the body of vertebrates, as comprehensive and diverse is the list of Axon Ligands™ interacting at all subtypes of dopaminergic receptors (selectively, or specific combinations).
Many 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)[2], and butyrophenones (haloperidol)[3]. Though still considered benchmark antipsychotics[4], they are known for there unwanted side effects such as dry mouth, extra pyramidal side effects, and tardive dyskinesia[5]. 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[6]. Among them, many Clozapine (Axon 1146) analogues, Aripiprazole (Axon 1143), and Ziprazidone (Axon 1446).
Dopamine receptor subtypes listed: D1, D2, D3, D4
[1] The Physiology, Signaling, and Pharmacology of Dopamine Receptors. J-M Beaulieu, R.R. Gainetdinov. Pharmacol. Rev. 2011, 63, 182-217.
[2] 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.
[3] Haloperidol: fifteen years of clinical experience. Ayd FJ. Diseases of the Nervous System 1972, 33, 459–69.
[4] Haloperidol versus chlorpromazine for treatment of schizophrenia. C. Leucht, M. Kitzmantel, L. Chua, J. Kane, and S. Leucht. Schizophr Bull 2008, 34, 813-815.
[5] Antipsychotics - the future of schizophrenia treatment. G. Beaumont. Curr Med Res Opin. 2000,16, 37-42.
[6] Side effects of atypical antipsychotics: a brief overview. A. Üçok and W. Gaebel. World Psychiatry. 2008, 7, 58–62.
Axon ID | Name | Description | From price | |
---|---|---|---|---|
2424 | WAY 100635 maleate | 5-HT1A antagonist with D4 agonistic properties | €125.00 | |
1086 | WAY 100635 hydrochloride | 5-HT1A antagonist | €125.00 | |
1060 | TL 99 hydrobromide | Dopamine agonist | €95.00 | |
1005 | TL 232 hydrobromide | Dopamine agonist | €95.00 | |
1004 | TL 102 hydrobromide | Dopamine agonist | €95.00 | |
2193 | Thioridazine hydrochloride | DA and α1 adrenoceptor antagonist; MALT1 inhibitor | €50.00 | |
2115 | Sonepiprazole hydrochloride | Selective dopamine D4 antagonist | €85.00 | |
1040 | Rotigotine | Dopamine agonist; more active enantiomer of N-0437 (Axon 1038) | €105.00 | |
1160 | R(-)-Norapomorphine hydrobromide | Dopamine agonist | €125.00 | |
1298 | Olanzapine | Atypical antipsychotic | €75.00 | |
1023 | N-Methyl-N-n-propyl-2-aminotetraline hydrochloride | Dopamine agonist | Inquire | |
1001 | N,N-Dipropyldopamine hydrobromide | Dopamine agonist | €95.00 | |
1061 | N,N-dibutyldopamine hydrobromide | Dopamine agonist | €95.00 | |
1039 | N 0924 hydrochloride | Dopamine agonist; less active enantiomer of N-0437 (Axon 1038) | Inquire | |
1041 | N 0734 hydrochloride | Dopamine agonist | €115.00 | |
1038 | N 0437 hydrochloride | Dopamine agonist | €135.00 | |
1065 | N 0426 hydrochloride | Dopamine agonist | Inquire | |
1063 | N 0425 hydrochloride, (-)- | MAO inhibitor | €135.00 | |
1062 | N 0425 hydrochloride, (+)- | MAO inhibitor | €135.00 | |
1022 | N 0425 hydrochloride | MAO inhibitor | €95.00 | |
1075 | MPTP hydrochloride | Dopamine neurotoxin | €80.00 | |
4004 | MPP+ iodide | Metabolite of MPTP (Axon 1075); Dopamine neurotoxin | €90.00 | |
1147 | Isoclozapine | Typical antipsychotic | €135.00 | |
1493 | Iloperidone | Atypical antipsychotic | €85.00 | |
3610 | Haloperidol | D2, D3 and D4 antagonist | €60.00 | |
1499 | Flibanserin | 5-HT1A agonist and 5-HT2A antagonist | €95.00 | |
1087 | Desmethyl-WAY 100635 trihydrochloride | Building Block for labelled 5-HT1A antagonist | €145.00 | |
1521 | CP 226269 | D4 agonist | €85.00 | |
1146 | Clozapine | Atypical antipsychotic | €50.00 | |
4357 | cis-(Z)-Flupenthixol dihydrochloride | Potent and selective DA receptor antagonist | Recently added | €130.00 |