Chemistry:UH-232
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Short description: Chemical compound
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| Formula | C18H29NO |
| Molar mass | 275.436 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] It 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 may also serve as a 5-HT2A receptor agonist, based on animal studies.[9] It was investigated in clinical trials for the treatment of schizophrenia, but unexpectedly caused symptoms to become worse.[9]
(+)-AJ76
The N-monopropyl derivative (+)-AJ76 is an active metabolite of UH-232 and has practically identical effects.
-AJ76_structure.png)
(+)-AJ76, CAS# 85378-82-1, 13755572
See also
References
- ↑ "The preferential dopamine D3 receptor ligand, (+)-UH232, is a partial agonist". European Journal of Pharmacology 282 (1–3): R3-4. August 1995. doi:10.1016/0014-2999(95)00460-3. PMID 7498261.
- ↑ "(+)-AJ 76 and (+)-UH 232: central stimulants acting as preferential dopamine autoreceptor antagonists". Naunyn-Schmiedeberg's Archives of Pharmacology 334 (3): 234–45. November 1986. doi:10.1007/BF00508777. PMID 2880302.
- ↑ "The dopamine D3 receptor and autoreceptor preferring antagonists (+)-AJ76 and (+)-UH232; a microdialysis study". European Journal of Pharmacology 242 (2): 151–63. September 1993. doi:10.1016/0014-2999(93)90075-S. PMID 8253112.
- ↑ "Dopamine D3-preferring ligands act at synthesis modulating autoreceptors". The Journal of Pharmacology and Experimental Therapeutics 274 (2): 609–13. August 1995. PMID 7636720.
- ↑ "Intracerebral infusion of (+)-AJ76 and (+)-UH232: effects on dopamine release and metabolism in vivo". European Journal of Pharmacology 251 (2–3): 181–90. January 1994. doi:10.1016/0014-2999(94)90399-9. PMID 8149975.
- ↑ "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 43 (3): 283–90. March 2001. doi:10.1006/phrs.2000.0773. PMID 11401421.
- ↑ "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. July 2004. doi:10.1007/s00213-003-1770-x. PMID 14985929.
- ↑ "Antagonism of cocaine's pharmacological effects by the stimulant dopaminergic antagonists, (+)-AJ76 and (+)-UH232". Brain Research 588 (2): 217–22. August 1992. doi:10.1016/0006-8993(92)91578-3. PMID 1393576.
- ↑ 9.0 9.1 "Effects of the D3 and autoreceptor-preferring dopamine antagonist (+)-UH232 in schizophrenia". Journal of Neural Transmission 105 (6–7): 719–34. 1998. doi:10.1007/s007020050091. PMID 9826114.
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