Imidazolines

Clonidine, sold under the brand name Catapres, Javadin, Kapvay among others, is an α2-adrenergic receptor agonist, hypotensive and anxiolytic drug used to treat high blood pressure, attention deficit hyperactivity disorder, perioperative pain, drug withdrawal (e.g., alcohol, opioids, or nicotine), and menopausal flushing. Clonidine is often prescribed off-label for tics. It is used orally (by mouth), by injection, or as a transdermal skin patch. Onset of action is typically within an hour with the effects on blood pressure lasting for up to eight hours. Xylazine is a structural analog of cloni

Levamisole, sold under the brand name Ergamisol among others, is a medication used to treat parasitic worm infections, specifically ascariasis and hookworm infections. It is taken by mouth.

Xylometazoline, also spelled xylomethazoline, is a medication used to reduce symptoms of nasal congestion, allergic rhinitis, and sinusitis. It is used directly in the nose as a spray or drops.

Imidacloprid is a systemic insecticide belonging to a class of chemicals called the neonicotinoids which act on the central nervous system of insects. The chemical works by interfering with the transmission of stimuli in the insect nervous system. Specifically, it causes a blockage of the nicotinergic neuronal pathway. By blocking nicotinic acetylcholine receptors, imidacloprid prevents acetylcholine from transmitting impulses between nerves, resulting in the insect's paralysis and eventual death. It is effective on contact and via stomach action. Because imidacloprid binds much more strongly

Tizanidine, sold under the brand name Zanaflex among others, is an alpha-2 (α2) adrenergic receptor agonist, similar to clonidine, that is used to treat muscle spasticity due to spinal cord injury, multiple sclerosis, and spastic cerebral palsy. Effectiveness appears similar to baclofen or diazepam. It is taken by mouth.

Naphazoline is a medicine used as a decongestant, and a vasoconstrictor added to eye drops to relieve red eye. It has a rapid action in reducing swelling when applied to mucous membranes. It is a sympathomimetic agent with marked alpha adrenergic activity that acts on alpha-receptors in the arterioles of the conjunctiva to produce constriction, resulting in decreased congestion.

Oxymetazoline, sold under the brand name Afrin among others, is a topical decongestant and vasoconstrictor medication. It is available over-the-counter as a nasal spray to treat nasal congestion and nosebleeds, as eye drops to treat eye redness due to minor irritation, and (in the United States) as a prescription topical cream to treat persistent facial redness due to rosacea in adults. Its effects begin within minutes and last for up to six hours. Intranasal use for longer than three to five days may cause congestion to recur or worsen, resulting in physical dependence. Fluticasone propionate

Phentolamine, sold under the brand name Regitine among others, is a non-selective α-adrenergic antagonist.

Tetryzoline (INN), also known as tetrahydrozoline, is a drug used in some over-the-counter eye drops and nasal sprays. Tetryzoline was patented in 1954, and came into medical use in 1959.

Brimonidine is an α2 agonist medication used to treat open-angle glaucoma, ocular hypertension, and rosacea. In rosacea it improves the redness. It is used as eye drops or applied to the skin. It is also available in the fixed-dose combination medication brimonidine/timolol along with timolol maleate.

Mazindol, sold under the brand names Mazanor and Sanorex, is an appetite suppressant which is used in the short-term treatment of obesity. It is also used off-label in the treatment of narcolepsy and cataplexy. The drug is taken orally.

Moxonidine (INN) is a new-generation alpha-2/imidazoline receptor agonist antihypertensive drug licensed for the treatment of mild to moderate essential hypertension. It may have a role when thiazides, beta-blockers, ACE inhibitors, and calcium channel blockers are not appropriate or have failed to control blood pressure. In addition, it demonstrates favourable effects on parameters of the insulin resistance syndrome, apparently independent of blood pressure reduction. It is also a growth hormone releaser. It is manufactured by Solvay Pharmaceuticals (acquired by Abbott in 2009) under the bran

2-Imidazoline (Preferred IUPAC name: '4,5-dihydro-1H-imidazole') is one of three isomers of the nitrogen-containing heterocycle imidazoline, with the formula C3H6N2. The 2-imidazolines are the most common imidazolines commercially, as the ring exists in some natural products and some pharmaceuticals. They also have been examined in the context of organic synthesis, coordination chemistry, and homogeneous catalysis.

Antazoline is a 1st generation antihistamine with anticholinergic properties used to relieve nasal congestion and in eye drops, usually in combination with naphazoline, to relieve the symptoms of allergic conjunctivitis. To treat allergic conjunctivitis, antazoline can be combined in a solution with tetryzoline. The drug is a Histamine H1 receptor antagonist: selectively binding to but not activating the receptor, thereby blocking the actions of endogenous histamine and subsequently leading to the temporary relief of the negative symptoms brought on by histamine.

Ergothioneine (EGT) is a naturally occurring amino acid and is a thiourea derivative of histidine, containing a sulfur atom on the imidazole ring. This compound occurs in relatively few organisms, notably actinomycetota, cyanobacteria, and certain fungi. Ergothioneine was discovered by Charles Tanret in 1909 and named after the ergot fungus from which it was first purified, with its structure being determined in 1911.

Imazapyr is a non-selective herbicide used for the control of a broad range of weeds including terrestrial annual and perennial grasses and broadleaved herbs, woody species, and riparian and emergent aquatic species.

Tolazoline is a non-selective competitive α2-adrenergic receptor antagonist. It is a vasodilator that is used to treat spasms of peripheral blood vessels (as in acrocyanosis). It has also been used (in conjunction with sodium nitroprusside) successfully as an antidote to reverse the severe peripheral vasoconstriction which can occur as a result of overdose with certain 5-HT2A receptor agonist drugs such as 25I-NBOMe, DOB, and Bromodragonfly. ==History== Tolazoline was first used in the 1980s as an alternative reversal agent for xylazine. ==Use== Tolazoline is used in large animal medicine to r

Lofexidine, sold as a generic by Indoco, MSN, Novitium, Ani Pharma, Regcon, etc; and under the brand name Lucemyra; is a medication historically used to treat high blood pressure; today, it is more commonly used to help with the physical symptoms of opioid withdrawal. It is taken by mouth. It is an α2A-adrenergic receptor agonist. It was initially approved for use by the Food and Drug Administration in the United States in 2018, considering it to be a first-in-class medication. Subsequent generic approvals by the FDA started August 21, 2024 with Indoco Remedies with Competitive Generic Therapy

chemical compound

Tramazoline is a chemical that is used in the form of tramazoline hydrochloride in nasal decongestant preparations. It is an α-adrenergic receptor agonist that inhibits secretion of nasal mucus.

chemical compound

Apraclonidine (INN), also known under the brand name Iopidine, is a sympathomimetic used in glaucoma therapy. It is an α2 adrenergic receptor agonist and a weak α1 adrenergic receptor agonist.

thumb|right|250px|Structures of 2-, 3-, and 4-imidazolines. Imidazoline is a heterocycle formally derived from imidazole by the reduction of one of the two double bonds. Three isomers are known, 2-imidazolines, 3-imidazolines, and 4-imidazolines. The 2- and 3-imidazolines contain an imine center, whereas the 4-imidazolines contain an alkene group. The 2-Imidazoline group occurs in several drugs.

Imidocarb is a urea derivative used in veterinary medicine as an antiprotozoal agent for the treatment of infection with Babesia (babesiosis) and other parasites.

Cirazoline is a full agonist at the α1A adrenergic receptor, a partial agonist at both the α1B and α1D adrenergic receptors, and a nonselective antagonist to the α2 adrenergic receptor. It is believed that this combination of properties could make cirazoline an effective vasoconstricting agent.

Fenobam is an imidazole derivative developed by McNeil Laboratories in the late 1970s as a novel anxiolytic drug with an at-the-time-unidentified molecular target in the brain. Subsequently, it was determined that fenobam acts as a potent and selective negative allosteric modulator of the metabotropic glutamate receptor subtype mGluR5, and it has been used as a lead compound for the development of a range of newer mGluR5 antagonists.

Romifidine is a drug that is used in veterinary medicine as a sedative mainly in large animals such as horses, although it may be used in a wide variety of species. It is not used in humans, but is closely related in structure to the commonly used drug clonidine.

Cibenzoline (or cifenline) is a Class Ia antiarrhythmic.

Nutlins are a family of small molecule, cis-imidazoline analogs, which inhibit the interaction between MDM2 and tumor suppressor p53, stabilizing p53 and triggering cell death and senescence. Three nutlins were discovered in the initial small molecule screen (nutlin-1, nutlin-2, and nutlin-3), but nutlin-3 is most commonly used in anti-cancer studies. Nutlins disrupt the p53–MDM2 interaction by occupying a p53-binding pocket of MDM2. Many tumors that express normal p53 and normal or elevated levels of MDM2 may be targeted using nutlin. Nutlin-3 acts quickly in vitro, leading to increased level

Dihydroimidazol-2-ylidene is a hypothetical organic compound with formula C3H6N2. It would be a heterocyclic compound, formally derived from imidazolidine with two hydrogen atoms removed from carbon number 2, leaving two vacant chemical bonds — which makes it a carbene.

Tolonidine is an antihypertensive. It is an imidazoline receptor agonist, like moxonidine and rilmenidine.

Indanidine is an alpha-adrenergic agonist.

Fenoxazoline (trade name Aturgyl in Brazil) is a nasal decongestant.

Efaroxan is an α2-adrenergic receptor antagonist and antagonist of the imidazoline receptor.

Tymazoline (trade name Thymazen in Poland) is a nasal decongestant that can be used to treat rhinitis. It acts as an antihistaminic and sympathomimetic, reducing swelling, inflammation and mucosal secretions.

Nepicastat (; developmental code names SYN117, RS-25560-197) is an inhibitor of dopamine β-hydroxylase (DBH), an enzyme that catalyzes the conversion of dopamine to norepinephrine.

Imiloxan is a drug which is used in scientific research. It acts as a selective antagonist for the α2B adrenergic receptor, and has been useful for distinguishing the actions of the different α2 adrenergic subtypes.

Tiamenidine (BAN, USAN, INN, also known as thiamenidine, Hoe 440) is an imidazoline compound that shares many of the pharmacological properties of clonidine. It is a centrally-acting α2 adrenergic receptor agonist (IC50 = 9.1 nM). It also acts as an α1-adrenergic receptor agonist to a far lesser extent (IC50 = 4.85 μM). In hypertensive volunteers, like clonidine, it significantly increased sinus node recovery time and lowered cardiac output. It was marketed (as tiamenidine hydrochloride) by Sanofi-Aventis under the brand name Sundralen for the management of essential hypertension.

Metizoline (trade name Ellsyl) is a nasal decongestant against allergic and vasomotor rhinitis.