Affinity profiles of various muscarinic antagonists for cloned human muscarinic acetylcholine receptor (mAChR) subtypes and mAChRs in rat heart and submandibular gland
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2019, Behavioural Brain ResearchSelective allosteric modulation of muscarinic acetylcholine receptors for the treatment of schizophrenia and substance use disorders
2019, Advances in PharmacologyCitation Excerpt :Binding studies using postmortem brain tissues from individuals with schizophrenia have also been used to assess alterations in the expression of different mAChRs, specifically M1 and/or M4. These studies were conducted by measuring changes in the binding of the M1-preferring orthosteric antagonist [3H]pirenzepine (relative binding affinity M1 > M4 > M2,3,5), under low doses thought to confer M1 specificity (Bolden, Cusack, & Richelson, 1992; Giachetti, Giraldo, Ladinsky, & Montagna, 1986; Moriya et al., 1999; Zang & Creese, 1997). In patients with schizophrenia compared to age-matched controls, these postmortem binding studies showed decreased levels of M1 in the prefrontal cortex (PFC), caudate putamen, hippocampus, and superior temporal gyrus (Crook et al.,1999; Crook, Tomaskovic-Crook, Copolov, & Dean, 2000, 2001; Dean et al., 1996; Dean, McLeod, Keriakous, McKenzie, & Scarr, 2002; Deng & Huang, 2005; Zavitsanou, Katsifis, Mattner, & Xu-Feng, 2004).