Cirazoline hydrochloride

Selective alpha1-adrenoceptor agonist; non-selective imidazoline binding site ligand

What it is

• Cirazoline (often used in its hydrochloride salt form) is a synthetic compound used in research settings (not a marketed therapeutic drug) that interacts with the adrenergic (and imidazoline) receptor systems. Wikipedia+3NCATS Inxight Drugs+3

• Its chemical description: for example, one source lists it as “2-(2-Cyclopropylphenoxymethyl)imidazoline hydrochloride”.

How it works (mechanism of action)

• Cirazoline acts as an agonist at the α₁-adrenergic receptor subtypes: specifically a full agonist at α₁A, and partial agonist at α₁B and α₁D. DrugBank+2IUPHAR/BPS Guide to PHARMACOLOGY+2

• It also acts as an antagonist (non-selective) at α₂-adrenergic receptors. PubMed+2NCATS Inxight Drugs+2

• Because of these receptor effects, it has been used as a tool compound to study how stimulation of α₁ and blockade of α₂ receptors influence physiological responses (e.g., vascular tone, feeding behavior, memory) in animals. Wikipedia+2PubMed+2

Functional (physiological) effects

• Vasoconstriction / blood-pressure effect: By stimulating α₁ receptors (which are often present on vascular smooth muscle), cirazoline can cause constriction of blood vessels and thereby increase blood pressure (in animal studies). DrugBank+1

• Impact on feeding / intake: In rats, cirazoline administered into the paraventricular nucleus of the hypothalamus reduced feeding and water intake, presumably via α₁-adrenoceptor activation. DrugBank+1

• Cognitive / memory effects: In aged rhesus monkeys, cirazoline impaired spatial working memory in certain tests, which suggests that α₁-adrenergic activation (or imidazoline receptor interaction) in the brain can affect prefrontal‐cortex-dependent functions. PubMed+1

Research / usage context

• It is primarily used as a research tool, not as an approved drug for treatment. DrugBank+1

• Many of the studies are in animals (rats, monkeys) or in vitro (cell membranes) rather than in humans.

• Being able to stimulate α₁A and partially α₁B/α₁D, and also block α₂, makes it useful for dissecting how different adrenergic receptor subtypes contribute to physiological responses.

Limitations & caveats

• Because the compound has multiple receptor activities (agonist at some, antagonist at others) and crosses into the brain, its effects can be complex and not purely selective. For example, interfering with memory in animals. PubMed+1

• The full safety, pharmacokinetics, metabolism, and human‐clinical profile are either not well characterized for therapeutic use.

• As with many experimental compounds, translation from animal studies to human set‐ups is uncertain.

0°C (short term), -20°C (long term), desiccated

1) Doze VA, et al. alpha(1A)- and alpha(1B)-adrenergic receptors differentially modulate antidepressant-like behaviorin the mouse.Brain Res. 2009 Aug 18;1285:148-57