UH-232
UH-232 ((+)-UH232) je lek koji deluje mešoviti agonist-antagonist dopaminskih receptora koji je selektivan za pojedine podtipove. On je slab parcijalni agonist na D3 podtipu,[1] i antagonist na D2Sh autoreceptorima u dopaminergičnim nervnim završecima.[2][3] On uzrokuje otpuštanje dopamina u mozgu i ima stimulišuče dejstvo.[4][5][6] On sprečava načina ponašanja koji je uzrokovan kokainom.[7] On je ispitivan za primenu u lečenju šizofrenije. Ispitivanja su prekinuta jer je pogoršavao simptome.[8]
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| IUPAC ime | |
|---|---|
cis-5-hidroksi-1-metil-2-(N,N-propilamino)tetralin | |
| Identifikatori | |
| CAS broj | 95999-12-5  |
| ATC kod | none |
| PubChem | CID 123696 |
| Hemijski podaci | |
| Formula | C18H29NO |
| Molarna masa | 275,428 g/mol |
| |
Reference
уреди- ^ Griffon N, Pilon C, Schwartz JC, Sokoloff P (1995). „The preferential dopamine D3 receptor ligand, (+)-UH232, is a partial agonist”. European journal of pharmacology. 282 (1–3): R3—4. PMID 7498261. doi:10.1016/0014-2999(95)00460-3.
- ^ Waters N, Lagerkvist S, Löfberg L, Piercey M, Carlsson A (1993). „The dopamine D3 receptor and autoreceptor preferring antagonists (+)-AJ76 and (+)-UH232; a microdialysis study”. European journal of pharmacology. 242 (2): 151—63. PMID 8253112. doi:10.1016/0014-2999(93)90075-S.
- ^ Aretha, CW; Sinha, A; Galloway, MP (1995). „Dopamine D3-preferring ligands act at synthesis modulating autoreceptors”. The Journal of pharmacology and experimental therapeutics. 274 (2): 609—13. PMID 7636720.
- ^ Waters, N; Hansson, L; Löfberg, L; Carlsson, A (1994). „Intracerebral infusion of (+)-AJ76 and (+)-UH232: effects on dopamine release and metabolism in vivo”. European journal of pharmacology. 251 (2–3): 181—90. PMID 8149975. doi:10.1016/0014-2999(94)90399-9.
- ^ Sotnikova, TD; Gainetdinov, RR; Grekhova, TV; Rayevsky, KS (2001). „Effects of intrastriatal infusion of D2 and D3 dopamine receptor preferring antagonists on dopamine release in rat dorsal striatum (in vivo microdialysis study)”. Pharmacological research : the official journal of the Italian Pharmacological Society. 43 (3): 283—90. PMID 11401421. doi:10.1006/phrs.2000.0773.
- ^ Millan, MJ; Seguin, L; Gobert, A; Cussac, D; Brocco, M (2004). „The role of dopamine D3 compared with D2 receptors in the control of locomotor activity: a combined behavioural and neurochemical analysis with novel, selective antagonists in rats”. Psychopharmacology. 174 (3): 341—57. PMID 14985929. doi:10.1007/s00213-003-1770-x.
- ^ Piercey, MF; Lum, JT; Hoffmann, WE; Carlsson, A; Ljung, E; Svensson, K (1992). „Antagonism of cocaine's pharmacological effects by the stimulant dopaminergic antagonists, (+)-AJ76 and (+)-UH232”. Brain research. 588 (2): 217—22. PMID 1393576. doi:10.1016/0006-8993(92)91578-3.
- ^ Lahti, AC; Weiler, M; Carlsson, A; Tamminga, CA (1998). „Effects of the D3 and autoreceptor-preferring dopamine antagonist (+)-UH232 in schizophrenia”. Journal of neural transmission (Vienna, Austria : 1996). 105 (6–7): 719—34. PMID 9826114. doi:10.1007/s007020050091.
