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. 

Items 31 to 49 of 49 total

per page
Page:
  1. 1
  2. 2
Axon ID Name Description From price
1062 N 0425 hydrochloride, (+)- MAO inhibitor €135.00
1063 N 0425 hydrochloride, (-)- MAO inhibitor €135.00
1065 N 0426 hydrochloride Dopamine agonist Inquire
1038 N 0437 hydrochloride Dopamine agonist €135.00
1041 N 0734 hydrochloride Dopamine agonist €115.00
1039 N 0924 hydrochloride Dopamine agonist; less active enantiomer of N-0437 (Axon 1038) Inquire
1061 N,N-dibutyldopamine hydrobromide Dopamine agonist €95.00
1001 N,N-Dipropyldopamine hydrobromide Dopamine agonist €95.00
1023 N-Methyl-N-n-propyl-2-aminotetraline hydrochloride Dopamine agonist Inquire
1298 Olanzapine Atypical antipsychotic €75.00
1160 R(-)-Norapomorphine hydrobromide Dopamine agonist €125.00
1040 Rotigotine Dopamine agonist; more active enantiomer of N-0437 (Axon 1038) €105.00
2115 Sonepiprazole hydrochloride Selective dopamine D4 antagonist €85.00
2193 Thioridazine hydrochloride DA and α1 adrenoceptor antagonist; MALT1 inhibitor €50.00
1004 TL 102 hydrobromide Dopamine agonist €95.00
1005 TL 232 hydrobromide Dopamine agonist €95.00
1060 TL 99 hydrobromide Dopamine agonist €95.00
1086 WAY 100635 hydrochloride 5-HT1A antagonist €125.00
2424 WAY 100635 maleate 5-HT1A antagonist with D4 agonistic properties €125.00

Items 31 to 49 of 49 total

per page
Page:
  1. 1
  2. 2
Please wait...