UH-232
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| Formula | C18H29NO |
| Molar mass | 275.428 g/mol g·mol−1 |
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UH-232 ((+)-UH232) is a drug which acts as a subtype selective mixed agonist-antagonist for dopamine receptors, acting as a weak partial agonist at the D3 subtype,[1] and an antagonist at D2Sh autoreceptors on dopaminergic nerve terminals.[2][3][4] This causes dopamine release in the brain and has a stimulant effect,[5][6][7] as well as blocking the behavioural effects of cocaine.[8] It was trialled for the treatment of schizophrenia but unexpectedly caused symptoms to become worse.[9]
See also
References
- ^ 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. doi:10.1016/0014-2999(95)00460-3. PMID 7498261.
- ^ Svensson, K.; Johansson, A. M.; Magnusson, T.; Carlsson, A. (1986). "(+)-AJ 76 and (+)-UH 232: Central stimulants acting as preferential dopamine autoreceptor antagonists". Naunyn-Schmiedeberg's Archives of Pharmacology. 334 (3): 234. doi:10.1007/BF00508777.
- ^ 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. doi:10.1016/0014-2999(93)90075-S. PMID 8253112.
- ^ 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. doi:10.1016/0014-2999(94)90399-9. PMID 8149975.
- ^ 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. doi:10.1006/phrs.2000.0773. PMID 11401421.
- ^ 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. doi:10.1007/s00213-003-1770-x. PMID 14985929.
- ^ 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. doi:10.1016/0006-8993(92)91578-3. PMID 1393576.
- ^ 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. doi:10.1007/s007020050091. PMID 9826114.