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SB-277011 GlaxoSmithKline.

G Remington¹, S Kapur

¹Center for Addiction and Mental Health, Toronto, Ontario, Canada. gary_remington@camh.net

Current Opinion in Investigational Drugs (London, England : 2000)

|January 5, 2002

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GlaxoSmithKline is investigating the dopamine D3 antagonist SB-277011 for schizophrenia treatment. This selective compound shows potential for psychosis and drug abuse, impacting the nucleus accumbens without causing catalepsy.

Area of Science:

Neuroscience
Pharmacology

Background:

GlaxoSmithKline is investigating the dopamine D3 antagonist SB-277011 and its analogs.
The compound's development follows the merger of Glaxo Wellcome and SmithKline Beecham.

Purpose of the Study:

To evaluate the potential of SB-277011 and related compounds in treating schizophrenia.
To explore their therapeutic roles in drug abuse and psychosis.

Main Methods:

Synthesis and evaluation of novel 2,3,4,5-tetrahydro-1H-benzazepines and 2,3-dihydro-1H-isoindoles.
Assessment of receptor affinity and selectivity for the dopamine D3 receptor.
Neurochemical analysis of D3 receptor blockade effects in the nucleus accumbens.

Main Results:

Related Experiment Videos

SB-277011 and analogs demonstrated high affinity and selectivity for the dopamine D3 receptor.

D3 receptor blockade with SB-277011 specifically altered neurochemical effects in the nucleus accumbens.

Unlike other antagonists, SB-277011 did not produce non-selective effects like catalepsy.

Conclusions:

SB-277011 shows promise as a selective dopamine D3 antagonist for treating schizophrenia.
The compound's targeted action suggests potential applications in managing drug abuse and psychosis.