Clonidine hydrochloride (C15-1238-569)

General description

Clonidine hydrochloride has antihypertensive analgesic and antidiarrheal properties. It lowers short-circuit current, blocks anion secretion, improves mucosal absorption of fluids and electrolytes in vitro. Clonidine is used to treat attention deficit and hyperactivity disorders (ADHD), menopausal flushing, drug withdrawal and Tourette′s syndrome.

Application

Clonidine hydrochloride has been used as an adrenergic receptor (ADRA2A) agonist:

• in ex vivo leptin release assay
• to study its effects on pain hypersensitivity in 6-OHDA lesioned rats
• to study its influence on the sleep of larval zebrafish
• to manipulate noradrenaline and examine its influence on behavioral flexibility and motivation

Clonidine hydrochloride has been used:

• to reduce central noradrenaline levels
• to inhibit allyl isothiocyanate (AITC) sensitized thermal aversion
• to attenuate thermal and mechanical pain hypersensitivity in rats
• as a positive control for pertussis toxin (PTX)

Biochem/physiol Actions

α₂-adrenoceptor agonist; I₁ imidazoline binding site ligand.

Clonidine hydrochloride is used for management of hypertension in pregnant women. In addition, it also acts as a therapeutic for neonatal abstinence syndrome. Clonidine hydrochloride binds to central α-adrenergic receptors and reduces the efferent sympathetic neuronal vasoconstrictor tone to the heart, kidneys and peripheral vasculature leading to vasodilatation and reduction in the blood pressure.

Features and Benefits

This compound is featured on the Imidazoline Binding Sites page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

This compound was developed by Boehringer Ingelheim. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.