A novel series of arylpiperazines with high affinity and selectivity for the dopamine D3 receptor

✍ Scribed by P. John Murray; Lee A. Harrison; Martin R. Johnson; Graeme M. Robertson; David I.C. Scopes; David R. Bull; Elizabeth A. Graham; Ann G. Hayes; Gavin J. Kilpatrick; Izaak Den Daas; Charles Large; Michael J. Sheehan; Carole M. Stubbs; Michael P. Turpin

• Publisher: Elsevier Science
• Year: 1995
• Tongue: English
• Weight: 210 KB
• Volume: 5
• Category: Article
• ISSN: 0960-894X
• DOI: 10.1016/0960-894x(95)00011-h

✦ Synopsis

A novel series of arylpiperazines has been synthesised which show high affinity for dopamine D 3 receptors. Several of these compounds exhibit ca. 100 fold selectivity for the dopamine D 3 receptor over D 1 , D 2 and D 4 receptors. In vivo studies suggest that 4 (GR103691) may have an atypical antipsychotic profile. Biochemical, pharmacological and, more recently, molecular biological studies have established that there is a family of at least five dopamine receptors: D 1 , D 2, D 3, D 4 and D5.1 Historically, the D 2 receptor has been the focus of therapeutic interest since antagonist activity at this receptor is a characteristic of most antipsychotics used in the treatment of schizophrenia. 2 However, the utility of standard antipsychotics is limited by extrapyramidal side-effects and by tardive dyskinesias, which