Cyprodime hydrochloride

Names

[ Name ]:
Cyprodime hydrochloride

Biological Activity

[Description]:

Cyprodime hydrochloride is a highly selective μ-opioid receptor antagonist with Ki values of 5.4 nM, 244.6 nM and 2187 nM for μ-, δ- and κ-opioid receptors, respectively. Cyprodime hydrochloride has anti-depressant-like effect[1][2].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Opioid Receptor

Signaling Pathways >> Neuronal Signaling >> Opioid Receptor

Research Areas >> Neurological Disease

[Target]

Ki: 5.4 nM (μ-opioid), 244.6 nM (δ-opioid) and 2187 nM (κ-opioid)[1]

[In Vitro]

Cyprodime hydrochloride has Ki values of 8.1 nM and 26.6 nM for μ-opioid receptor in rat brain (Wistar) and guinea pig brain[1].

[In Vivo]

Cyprodime hydrochloride (3, 10 mg/kg; i.p.; 60 min prior to test) significantly increases immobility time in the forced swimming test (FST) with higher dose of 10 mg/kg. Cyprodime hydrochloride increases the grooming time[2]. Animal Model: Male NMRI mice aged 21-25 days and weighing 10-12 g[2] Dosage: 3, 10 mg/kg Administration: IP; 60 min prior to test Result: Significantly increased immobility time in the forced swimming test (FST) with higher dose of 10 mg/kg.

[References]

[1]. Márki A, et al. Mu-opioid receptor specific antagonist cyprodime: characterization by in vitro radioligand and [³⁵S]GTPgammaS binding assays. Eur J Pharmacol. 1999 Oct 27;383(2):209-14.

[2]. Haj-Mirzaian A, et al. Involvement of opioid system in behavioral despair induced by social isolation stress in mice. Biomed Pharmacother. 2019 Jan;109:938-944.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₂H₃₀ClNO₃

[ Molecular Weight ]:
391.93

Related Compounds

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