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Odapipam

Names

[ CAS No. ]:
131796-63-9

[ Name ]:
Odapipam

[Synonym ]:
Odapipam
Nnc 756
UNII-847PQF7ZN6

Biological Activity

[Description]:

Odapipam (NNC 756) is a selective, high affinity and benzazepine dopamine D1 receptor antagonist with a Kd of 0.18 nM. Odapipam is also a superior positron emission tomography (PET) radiotracer[1][2].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor
Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor
Research Areas >> Neurological Disease

[Target]

Dopamine D1 receptor[1]


[In Vivo]

The metabolism of Odapipam has been studied with phenobarbital-induced rat liver microsomes. During the incubation of Odapipam, five different metabolites are formed. The electron-ionization (EI+) mass spectra of the metabolites indicated the formation of N-desmethyl-Odapipam, 1-hydroxy-Odapipam, the two isomers of 3′-hydroxy-Odapipam and a metabolite which is dehydrogenated in the dihydrobenzofuran moiety[3].

[References]

[1]. Abi-Dargham A, et al. PET studies of binding competition between endogenous dopamine and the D1 radiotracer [11C]NNC 756. Synapse. 1999 May;32(2):93-109.

[2]. Nielsen EB, et al. Dopamine receptor occupancy in vivo: behavioral correlates using NNC-112, NNC-687 and NNC-756, new selective dopamine D1 receptor antagonists. Eur J Pharmacol. 1992 Aug 14;219(1):35-44.

[3]. J. VANGGAARD ANDERSEN, et al. Normal-phase liquid chromatography-particle-beam mass spectrometry in drug metabolism studies of the dopamine receptor antagonist Odapipam and the muscarine M1 receptor agonist Xanomeline. Xenobiotica. 1997, 27: 901-912.

Chemical & Physical Properties

[ Density]:
1.269g/cm3

[ Boiling Point ]:
460.4ºC at 760mmHg

[ Molecular Formula ]:
C19H20ClNO2

[ Molecular Weight ]:
329.82100

[ Flash Point ]:
232.2ºC

[ Exact Mass ]:
329.11800

[ PSA ]:
32.70000

[ LogP ]:
3.53820

[ Vapour Pressure ]:
4.27E-09mmHg at 25°C

[ Index of Refraction ]:
1.623

Safety Information

[ HS Code ]:
2934999090

Customs

[ HS Code ]: 2934999090

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%


Related Compounds