PNU-99,194

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PNU-99,194
PNU-99194A-structure.png
Systematic (IUPAC) name
5,6-dimethoxy-N,N-dipropyl-2,3-dihydro-1H-inden-2-amine
Clinical data
Legal status
  • Uncontrolled
Routes of
administration		 Oral
Identifiers
CAS Number 82668-33-5
Template:CAS (maleate)
Template:CAS (hydrochloride)
ATC code none
PubChem CID: 5626
ChemSpider 5424
ChEMBL CHEMBL16410
Chemical data
Formula C17H27NO2
Molecular mass 277.40 g/mol
  • O(c1cc2c(cc1OC)CC(N(CCC)CCC)C2)C

PNU-99,194(A) (or U-99,194(A)) is a drug which acts as a moderately selective D3 receptor antagonist with ~15-30-fold preference for D3 over the D2 subtype.[1][2][3] Though it has substantially greater preference for D3 over D2, the latter receptor does still play some role in its effects, as evidenced by the fact that PNU-99,194 weakly stimulates both prolactin secretion and striatal dopamine synthesis, actions it does not share with the more selective (100-fold) D3 receptor antagonists S-14,297 and GR-103,691.[4]

In rodent studies, low doses of PNU-99,194 produce conditioned place preference (CPP) with no effect on intracranial self-stimulation (ICSS), whereas low doses of D3 agonists like 7-OH-DPAT inhibit ICSS behavior and cause conditioned place aversion (CPA).[5][6][7] In contrast, high doses of PNU-99,194 produce CPA and inhibit ICSS, while high doses of 7-OH-DPAT result in the opposite.[5][6][7] Paralleling this, low doses of PNU-99,194 and 7-OH-DPAT induce hyperactivity and hypoactivity, respectively, whereas the inverse is seen at high doses with both agents.[2][3][7][8][9][10] These data indicate that the D3 receptor has biphasic effects on reward mechanisms and locomotor activity, likely due to opposing roles of autoreceptors versus postsynaptic receptors.[8][11]

Other effects of PNU-99,194 at low doses in rodents include increased nociceptive responses,[12] hypothermia,[4][13] anxiolysis,[14] and facilitation of learning and memory,[12][15][16][17] as well as augmentation and inhibition, respectively, of amphetamine-induced reward and behavioral sensitization,[18][19] and reversal of morphine-induced CPP.[6] At high doses it inhibits the self-administration of cocaine in both rats and monkeys.[1][20]

See also

References

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  8. ↑ 8.0 8.1 Lua error in package.lua at line 80: module 'strict' not found.
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  13. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  14. ↑ Lua error in package.lua at line 80: module 'strict' not found.
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  20. ↑ Lua error in package.lua at line 80: module 'strict' not found.
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