ACADIA Pharmaceuticals Inc.

About: ACADIA Pharmaceuticals Inc. is a company organization based out in San Diego, California, United States. It is known for research contribution in the topics: Pimavanserin & Receptor. The organization has 260 authors who have published 276 publications receiving 8418 citations.

Should inverse agonists be defined by pharmacological mechanism or clinical effect

Abstract: Pimavanserin was recently approved for treating hallucinations and delusions associated with Parkinson’s disease.1 It is the first approved drug that selectively targets the 5-HT2A receptor and is termed a selective serotonin inverse agonist. This has motivated a debate about which drugs should be classified as inverse agonists – those that display clear evidence of inverse agonist activity in vitro, or only those that have demonstrated clinical evidence of inverse agonism.2 This is a valid question. Here I advance the view that drugs are defined by their in vitro pharmacological profiles and mechanisms of action to the extent that these mechanisms are understood. Constitutive receptor activity and inverse agonism are now well-defined pharmacological properties, documented at the structural level. Therefore, calling pimavanserin an inverse agonist based on its molecular pharmacology properties is appropriate.

Solid phase parallel synthesis of tertiary amines

Abstract: Described is method for preparing tertiary amines comprising sequential, exhaustive alkylation of a hydroxylamine derivative and cleavage of the O-N bond using the following steps: (a) reacting the hydroxylamine derivative with an alkylating agent or with a carbonyl compound to form an oxime intermediate; (b) reacting the oxime intermediate with a reducing agent to produce an alkylated derivative; (c) reacting the alkylated derivative with an alkylating agent or a carbonyl compound in the presence of a reducing agent to produce a dialkylated derivative; (d) reacting the dialkylated derivative with an alkylating agent to produce a quaternized derivative; (e) reacting the quaternized derivative with a reagent causing cleavage of the O-N bond to produce a tertiary amine.