Target intelligence / Profile preview

Phosphodiesterase (particularly PDE10A) (PDE (or PDE10A for specificity))

Target
PDE (or PDE10A for specificity)
Molecular classification
Enzyme, Other (for calcium channel blockade, though not the primary molecular target)
01

Overview

Papaverine is an opium alkaloid used clinically as a direct smooth muscle relaxant. Its primary molecular target is phosphodiesterase enzymes (notably PDE10A), whose inhibition increases intracellular levels of cAMP and cGMP, disrupting pathways required for sustained muscle contraction. Papaverine also blocks calcium ion channels, further decreasing calcium-dependent contractility. These mechanisms allow papaverine to treat vascular, visceral, and urological spasms. Although it is not structurally related to other opium alkaloids, its unique effects on smooth muscle contraction underpin its clinical utility. Some studies suggest papaverine can affect mitochondrial respiration, offering a secondary route for muscle relaxation in certain tissues.

Other names
PhosphodiesterasecAMP phosphodiesterasecGMP phosphodiesterasePDE10A
02

Mechanism of action

Inhibition of phosphodiesterase (especially PDE10A), resulting in increased intracellular cAMP and cGMP levels, causing smooth muscle relaxation. Blockade of calcium ion channels, reducing calcium influx and release, thereby further decreasing contraction. Inhibition of mitochondrial respiration (secondary mechanism in some tissues).

03

Biological functions

Regulation of intracellular cyclic nucleotide levels (cAMP and cGMP)Modulation of smooth muscle contractionSignal transduction
04

Disease associations

Cardiovascular disease (vasospasm, angina pectoris)Gastrointestinal spasmUrological spasmImpotenceOther (antipsychotic effects have been studied, but not confirmed)
05

Safety considerations

Hypotension due to excessive vasodilationHepatic toxicityCNS side effects (motor and cognitive deficits observed in preclinical studies with chronic use)
06

Interacting drugs

Papaverine

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