D2

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. 

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Axon ID Name Description From price
1035 PPHT hydrochloride D2 agonist €140.00
1579 Pridopidine hydrochloride Dopaminergic stabilizer that stabilizes psychomotor activity €140.00
1354 Quetiapine fumarate Atypical antipsychotic €75.00
1162 R(-)-N-Ethylnorapomorphine hydrochloride D2 agonist Inquire
1161 R(-)-N-Propylnorapomorphine hydrobromide D2 agonist €140.00
1160 R(-)-Norapomorphine hydrobromide Dopamine agonist €125.00
1454 Risperidone Atypical antipsychotic €75.00
1040 Rotigotine Dopamine agonist; more active enantiomer of N-0437 (Axon 1038) €105.00
1003 RU 24213 D2 agonist €105.00
1141 Sertindole 5-HT2, D2 and α1 adrenoceptor antagonist €82.00
1342 ST 148 D2 antagonist €115.00
1519 Sunepitron hydrochloride Anxiolytic and antidepressant drug €140.00
1144 Thio-aripiprazole Atypical antipsychotic €140.00
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
2562 UNC9994 hydrochloride β-Arrestin-biased functionally selective dopamine D2R agonist €120.00
1446 Ziprasidone hydrochloride Atypical antipsychotic €50.00

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