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UH-232
Systematic (IUPAC) name
cis-5-hydroxy-1-methyl-2-(N,N-propylamino)tetralin
Identifiers
CAS number 95999-12-5
ATC code none
PubChem 123696
Chemical data
Formula C18H29NO 
Mol. mass 275.428 g/mol
SMILES eMolecules & PubChem
Therapeutic considerations
Pregnancy cat.  ?
Legal status

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] This causes dopamine release in the brain and has a stimulant effect,[4][5][6] as well as blocking the behavioural effects of cocaine.[7] It was trialled for the treatment of schizophrenia but unexpectedly caused symptoms to become worse.[8]

See also

References

  1. ^ Griffon N, Pilon C, Schwartz JC, Sokoloff P. The preferential dopamine D3 receptor ligand, (+)-UH232, is a partial agonist. European Journal of Pharmacology. 1995 Aug 25;282(1-3):R3-4. PMID 7498261
  2. ^ Waters N, Lagerkvist S, Löfberg L, Piercey M, Carlsson A. The dopamine D3 receptor and autoreceptor preferring antagonists (+)-AJ76 and (+)-UH232; a microdialysis study. European Journal of Pharmacology. 1993 Sep 28;242(2):151-63. PMID 8253112
  3. ^ Aretha CW, Sinha A, Galloway MP. Dopamine D3-preferring ligands act at synthesis modulating autoreceptors. Journal of Pharmacology and Experimental Therapeutics. 1995 Aug;274(2):609-13. PMID 7636720
  4. ^ Waters N, Hansson L, Löfberg L, Carlsson A. Intracerebral infusion of (+)-AJ76 and (+)-UH232: effects on dopamine release and metabolism in vivo. European Journal of Pharmacology. 1994 Jan 14;251(2-3):181-90. PMID 8149975
  5. ^ Sotnikova TD, Gainetdinov RR, Grekhova TV, Rayevsky KS. 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. 2001 Mar;43(3):283-90. PMID 11401421
  6. ^ Millan MJ, Seguin L, Gobert A, Cussac D, Brocco M. 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 (Berlin). 2004 Jul;174(3):341-57. PMID 14985929
  7. ^ Piercey MF, Lum JT, Hoffmann WE, Carlsson A, Ljung E, Svensson K. Antagonism of cocaine's pharmacological effects by the stimulant dopaminergic antagonists, (+)-AJ76 and (+)-UH232. Brain Research. 1992 Aug 21;588(2):217-22. PMID 1393576
  8. ^ Lahti AC, Weiler M, Carlsson A, Tamminga CA. Effects of the D3 and autoreceptor-preferring dopamine antagonist (+)-UH232 in schizophrenia. Journal of Neural Transmission. 1998;105(6-7):719-34. PMID 9826114
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