title: SB-277011 GlaxoSmithKline.
abstract: It is presumed that GlaxoSmithKline has taken over from SmithKline Beecham in investigating the highly selective dopamine D3 antagonist SB-277011 and its analogs for the potential treatment of schizophrenia [284490] following the merger of Glaxo Wellcome and SmithKline Beecham in December 2000 [394715]. In June 2000, it was reported that novel 2,3,4,5-tetrahydro-1H-benzazepines and 2,3-dihydro-1H-isoindoles, including SB-277011, had shown high affinity and selectivity for the dopamine D3 receptor. All compounds were suggested to have further potential roles in the treatment of drug abuse and psychosis [372205]. In November 2000, data presented at the 30th Neuroscience meeting in New Orleans, LA, demonstrated that D3 receptor blockade with SB-277011 specifically altered neurochemical effects in the nucleus accumbens without the non-selective effects, such as catalepsy, seen with some other antagonists [390460].
authors.affiliation: Center for Addiction and Mental Health, Toronto, Ontario, Canada. gary_remington@camh.net
authors.forename: G
authors.initials: G
authors.lastname: Remington
authors.forename: S
authors.initials: S
authors.lastname: Kapur
mesh_terms: D000818:Animals; D014150:Antipsychotic Agents / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology*; D018492:Dopamine Antagonists / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology*; D065127:Dopamine D2 Receptor Antagonists; D004353:Drug Evaluation, Preclinical; D008032:Limbic System / Q000378:metabolism; D009570:Nitriles / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology*; D011804:Quinolines / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology*; D051381:Rats; D017448:Receptors, Dopamine D2 / Q000378:metabolism / Q000502:physiology; D050637:Receptors, Dopamine D3; D013329:Structure-Activity Relationship; D044005:Tetrahydroisoquinolines
chemical_list: D014150:Antipsychotic Agents; D018492:Dopamine Antagonists; D065127:Dopamine D2 Receptor Antagonists; C493595:Drd3 protein, rat; D009570:Nitriles; D011804:Quinolines; D017448:Receptors, Dopamine D2; D050637:Receptors, Dopamine D3; C409982:SB 277011; D044005:Tetrahydroisoquinolines