Chemistry:Odapipam

From HandWiki

Odapipam (INN; developmental code names NNC 01-0756, NNC-756, NO-756) is a selective D1 receptor antagonist of the benzazepine group which was investigated as a potential antipsychotic but was never marketed.[1][2]

It has more than 5,000-fold selectivity for the dopamine D1 receptor (Ki = 0.17 nM) over the dopamine D2 receptor (Ki = 942 nM).[3] Its affinities for other dopamine receptors, such as the dopamine D5 receptor, were not reported.[3][4] In addition to the dopamine D1 receptor, odapipam showed relatively high affinity for the serotonin 5-HT2 receptor (Ki = 4.5 nM; 26-fold lower than for the D1 receptor).[4]

The drug was first described in the scientific literature by 1988.[4][5]

See also

  • Substituted 3-benzazepine
  • Berupipam (NNC 22-0010)
  • Ecopipam (SCH-39166)
  • NNC 01-0687 (ADX-10061)
  • SCH-23390

References

  1. ↑ "A history of antipsychotic drug development". Compr Psychiatry 40 (6): 407–414. 1999. doi:10.1016/s0010-440x(99)90082-2. PMID 10579370. 
  2. ↑ "The principal features and mechanisms of dopamine modulation in the prefrontal cortex". Prog Neurobiol 74 (1): 1–58. September 2004. doi:10.1016/j.pneurobio.2004.05.006. PMID 15381316. 
  3. ↑ 3.0 3.1 "Role of Dopamine in the Heart in Health and Disease". Int J Mol Sci 24 (5): 5042. March 2023. doi:10.3390/ijms24055042. PMID 36902474. 
  4. ↑ 4.0 4.1 4.2 "NNC-112, NNC-687 and NNC-756, new selective and highly potent dopamine D1 receptor antagonists". Eur J Pharmacol 219 (1): 45–52. August 1992. doi:10.1016/0014-2999(92)90578-r. PMID 1397049. 
  5. ↑ "Functional interactions between D-1 and D-2 dopamine receptor systems: their role in the regulation of psychomotor behaviour, putative mechanisms, and clinical relevance". J Psychopharmacol 3 (2): 54–63. January 1989. doi:10.1177/026988118900300202. PMID 22156499. 




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