70824-86-1

Usage

Uses

Used in Pharmaceutical Research:
1-FLUORO-3-PHENYLPROPAN-2-AMINE is used as a research compound for studying the effects of fluorinated amphetamines on neurotransmitter release in the striatum of the rat. This application aids in understanding the underlying mechanisms of action and potential therapeutic applications of this class of compounds.
Used in Neurotransmission Modulation:
1-FLUORO-3-PHENYLPROPAN-2-AMINE is used as a modulator of neurotransmission for investigating its potential effects on the release of putative neurotransmitter amines in the striatum of the rat. This application can provide insights into the compound's influence on neuronal signaling and its possible use in the development of drugs targeting specific neurological conditions.

Upstream product

• 503-20-8 fluoroacetonitrile 
• 6921-34-2 benzylmagnesium chloride 
• 336783-89-2 (2-azido-3-fluoro-propyl)benzene 

Relevant academic research and scientific papers

Positive modulators of nicotinic receptor agonists

Compounds according to formula I: wherein R1, W, R2, R3, X, R4 and R5 are as described in the specification, enantiomers thereof, pharmaceutically acceptable salts thereof, processes for preparing the

Synthesis and biochemical evaluation of 3-fluoromethyl-1,2,3,4- tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N- methyltransferase versus the α2-adrenoceptor

A series of 3-fluoromethyl-1,2,3,4-tetrahydroisoquinolines (3- fluoromethyl-THIQs) was proposed, and their phenylethanolamine N- methyltransferase (PNMT) and α2-adrenoceptor affinities were predicted through the use of comparative molecular field analysis (CoMFA) models. These compounds were synthesized and evaluated for affinity at PNMT and the α2- adrenoceptor. It was discovered that these compounds are some of the most selective inhibitors of PNMT versus the α2-adrenoceptor known. To determine the ability of these compounds to penetrate the blood-brain barrier (BBB), a series of THIQs possessing a variety of calculated partition coefficients (Clog P) were assayed using an in vitro BBB model. This study found a good correlation between lipophilicity (Clog P) and BBB permeability, which indicated that THIQs possessing Clog P values of at least 0.13-0.57 should have some penetration into the brain. Two compounds [3-fluoromethyl-7-N-(4- chlorophenyl)aminosulfonyl-THIQ (18) and 3-fluoromethyl-7-cyano-THIQ (20)] possess calculated partition coefficients greater than 0.57 and display selectivities (α2-adrenoceptor K/PNMT K1) greater than 200 and thus represent promising leads in the development of highly selective inhibitors of PNMT with the ability to penetrate the BBB.