Movatterモバイル変換

[0]ホーム
URL:

Jump to content
WikipediaThe Free Encyclopedia
Search

Odapipam

From Wikipedia, the free encyclopedia
Abandoned D1 receptor antagonist
Pharmaceutical compound
Odapipam
Clinical data
Other namesNNC 01-0756; NNC-01-0756; NNC-010756; NNC010756; NNC01-0756; NNC-756; NNC756; NNC 0756; NNC0756; NO-756; NO756
Drug classDopamineD1 receptorantagonist
Identifiers
  • (5S)-8-chloro-5-(2,3-dihydro-1-benzofuran-7-yl)-3-methyl-1,2,4,5-tetrahydro-3-benzazepin-7-ol
CAS Number
PubChemCID
ChemSpider
UNII
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC19H20ClNO2
Molar mass329.82 g·mol−1
3D model (JSmol)
  • CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC=CC4=C3OCC4)O)Cl
  • InChI=1S/C19H20ClNO2/c1-21-7-5-13-9-17(20)18(22)10-15(13)16(11-21)14-4-2-3-12-6-8-23-19(12)14/h2-4,9-10,16,22H,5-8,11H2,1H3/t16-/m1/s1
  • Key:SKMVRXPBCSTNKE-MRXNPFEDSA-N

Odapipam (INNTooltip International Nonproprietary Name; developmental code namesNNC 01-0756,NNC-756,NO-756) is aselectiveD1 receptorantagonist of thebenzazepine group which was investigated as a potentialantipsychotic 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 dopamineD2 receptor (Ki = 942 nM).[3] Itsaffinities for otherdopamine receptors, such as the dopamineD5 receptor, were not reported.[3][4] In addition to the dopamine D1 receptor, odapipam showed relatively high affinity for theserotonin5-HT2 receptor (Ki = 4.5 nM; 26-fold lower than for the D1 receptor).[4]

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

See also

[edit]

References

[edit]
  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. ^abNeumann 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. ^abcAndersen 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.
D1-like
Agonists
PAMs
Antagonists
D2-like
Agonists
Antagonists
5-HT1
5-HT1A
5-HT1B
5-HT1D
5-HT1E
5-HT1F
5-HT2
5-HT2A
5-HT2B
5-HT2C
5-HT3–7
5-HT3
5-HT4
5-HT5A
5-HT6
5-HT7


Stub icon

Thispsychoactive drug-related article is astub. You can help Wikipedia byexpanding it.

Retrieved from "https://en.wikipedia.org/w/index.php?title=Odapipam&oldid=1316585966"
Categories:
Hidden categories:
[8]ページ先頭
©2009-2025 Movatter.jp