Odapipam (INNTooltip International Nonproprietary Name; 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

References

  1. ^ Shen WW (1999). "A history of antipsychotic drug development". Compr Psychiatry. 40 (6): 407–414. doi:10.1016/s0010-440x(99)90082-2. PMID 10579370.
  2. ^ Seamans JK, Yang CR (September 2004). "The principal features and mechanisms of dopamine modulation in the prefrontal cortex". Prog Neurobiol. 74 (1): 1–58. doi:10.1016/j.pneurobio.2004.05.006. PMID 15381316.
  3. ^ a b Neumann J, Hofmann B, Dhein S, Gergs U (March 2023). "Role of Dopamine in the Heart in Health and Disease". Int J Mol Sci. 24 (5): 5042. doi:10.3390/ijms24055042. PMC 10003060. PMID 36902474.
  4. ^ a b c Andersen PH, Grønvald FC, Hohlweg R, Hansen LB, Guddal E, Braestrup C, Nielsen EB (August 1992). "NNC-112, NNC-687 and NNC-756, new selective and highly potent dopamine D1 receptor antagonists". Eur J Pharmacol. 219 (1): 45–52. doi:10.1016/0014-2999(92)90578-r. PMID 1397049.
  5. ^ Waddington JL (January 1989). "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. doi:10.1177/026988118900300202. PMID 22156499.


Allikas: https://en.wikipedia.org/wiki/Odapipam
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