Drug intelligence / Profile preview

1-phenylpiperazine

Development stage
Unknown
Modality
Small Molecules
01

Overview

1-Phenylpiperazine is a simple chemical compound consisting of a phenyl group bound to a piperazine ring. It serves as the parent structure for a wide range of bioactive derivatives known as substituted phenylpiperazines. Pharmacologically, it acts primarily as a monoamine releasing agent with modest selectivity for norepinephrine over serotonin and dopamine. Its EC50 values indicate it is about five times more potent at releasing norepinephrine than serotonin and over thirteen times more potent than dopamine release. The compound itself has limited direct therapeutic use but is widely utilized in pharmaceutical research and drug development as an intermediate or reference standard. It also plays roles in neurotransmitter research (notably involving serotonin and dopamine receptors), behavioral studies in animal models related to psychoactive substances and addiction mechanisms, analytical chemistry (as a standard), and material science applications[2][6][7]. At high doses it can be toxic; its oral LD50 in rats is reported at 210 mg/kg[2].

Other names
phenylpiperazineN-phenylpiperazine4-phenylpiperazineVortioxetine impurity A1-fenylpiperazinAKOS BBS-00003581
02

Targets

SERT (Sodium-dependent serotonin transporter)NET (Norepinephrine Transporter)DAT (Dopamine plasma membrane transport protein)

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