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Restrict the search for
acetylcholine
to a specific field?
Status:
US Previously Marketed
First marketed in 1933
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Piperocaine (Metycaine) is a local anesthetic drug. It is an ester and primarily is a sodium channel blocker. Piperocaine can partially inhibit dopamine. It is known as a alpha-1-proteinase inhibitor. Used in the form of its hydrochloride as a local or spinal anesthetic and in dental anesthesia. Can cause toxic reactions. Piperocaine Hydrochloride is in the list of Bulk Drug Substances Nominated for Use in Compounding Under Section 503A, FDA Act. Piperocaine hydrochloride is a small, white odorless crystals or a white crystalline powder, stable in air, freely soluble in water, alcohol and chloroform.
Status:
US Previously Marketed
Source:
Hydrochloric Acid U.S.P.
(1921)
Source URL:
First marketed in 1921
Source:
Hydrochloric Acid U.S.P.
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
HYDROCHLORIC ACID is formed by dissolving hydrogen chloride gas in water. It is a strong corrosive acid that is commonly used as a laboratory reagent. Also, it constitutes the majority of gastric acid, the human digestive fluid. Skin contact with HYDROCHLORIC ACID can cause redness, pain, and severe skin burns. It may cause severe burns to the eye and permanent eye damage.
Status:
US Previously Marketed
Source:
Homatropine Hydrobromide U.S.P.
(1921)
Source URL:
First marketed in 1921
Source:
Homatropine Hydrobromide U.S.P.
Source URL:
Class (Stereo):
CHEMICAL (EPIMERIC)
Conditions:
Homatropine (used in a form of bromide or methylbromide salts) is an analogue of atropine, which acts as an antagonist of muscarinic receptors. Homatropine was approved for the treatment of cough in combination with hydrocodone bitartrate.
Status:
US Previously Marketed
Source:
Hyoscyamine Hydrobromide U.S.P.
(1921)
Source URL:
First marketed in 1921
Source:
Hyoscyamine Hydrobromide U.S.P.
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Hyoscyamine as a natural plant alkaloid derivative and anticholinergic. Hyoscyamine is used to treat a variety of stomach/intestinal problems such as cramps and irritable bowel syndrome. It is also used to treat other conditions such as bladder and bowel control problems, cramping pain caused by kidney stones and gallstones, and Parkinson's disease. In addition, it is used to decrease side effects of certain medications (drugs used to treat myasthenia gravis) and insecticides. Hyoscyamine inhibits specifically the actions of acetylcholine on structures innervated by postganglionic cholinergic nerves and on smooth muscles that respond to acetylcholine but lack cholinergic innervation. These peripheral cholinergic receptors are present in the autonomic effector cells of the smooth muscle, cardiac muscle, the sinoatrial node, the atrioventricular node, and the exocrine glands. At therapeutic doses, it is completely devoid of any action on autonomic ganglia. Side effects include dry mouth and throat, increased appetite leading to weight gain, eye pain, blurred vision, restlessness, dizziness, arrhythmia, flushing, and faintness. Additive adverse effects resulting from cholinergic blockade may occur when hyoscyamine is administered concomitantly with other antimuscarinics, amantadine, haloperidol, phenothiazines, monoamine oxidase (MAO) inhibitors, tricyclic antidepressants or some antihistamines.
Status:
US Previously Marketed
First marketed in 1911
Class (Stereo):
CHEMICAL (EPIMERIC)
Methylatropine (methylatroponium) is a belladonna derivative. In 1902 the Bayer Company introduced atropine methonitrate, a quaternary ammonium salt of atropine (Eumydrin), as a mydriatic for dilation of the pupil during ophthalmic examination. Due to its highly polar nature it penetrates less readily into the central nervous system than atropine and was therefore introduced for relieving pyloric spasms in infants. Atropine methyl nitrate is a muscarinic acetylcholine receptor antagonist that does not cross the blood-brain barrier. Atropine methyl nitrate has been used for its peripheral muscarinic effects (targeting the bladder, respiratory tract, and to block parasympathetic signaling to the heart, among others) and to separate central from peripheral nervous system effects, or to protect against peripheral side effects when using muscarinics that do cross the blood brain barrier.
Status:
US Previously Marketed
Source:
PROCAINE HYDROCHLORIDE by GD SEARLE LLC
(1982)
Source URL:
First marketed in 1905
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Procaine is an anesthetic agent indicated for production of local or regional anesthesia, particularly for oral surgery. Procaine (like cocaine) has the advantage of constricting blood vessels which reduces bleeding, unlike other local anesthetics like lidocaine. Procaine is an ester anesthetic. It is metabolized in the plasma by the enzyme pseudocholinesterase through hydrolysis into para-aminobenzoic acid (PABA), which is then excreted by the kidneys into the urine. Procaine acts mainly by inhibiting sodium influx through voltage gated sodium channels in the neuronal cell membrane of peripheral nerves. When the influx of sodium is interrupted, an action potential cannot arise and signal conduction is thus inhibited. The receptor site is thought to be located at the cytoplasmic (inner) portion of the sodium channel. Procaine has also been shown to bind or antagonize the function of N-methyl-D-aspartate (NMDA) receptors as well as nicotinic acetylcholine receptors and the serotonin receptor-ion channel complex.
Status:
US Previously Marketed
Source:
Bantron by Campana
(1953)
Source URL:
First marketed in 1882
Source:
Lobeline Sulphate by E. Merck
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Lobeline is an alkaloid found in "Indian tobacco" (Lobelia inflata), "Devil's tobacco" (Lobelia tupa), "cardinal flower" (Lobelia cardinalis), "great lobelia" (Lobelia siphilitica), and Hippobroma longiflora. Additionally, it is also found in Lobelia Chinensis. In its pure form, it is a white amorphous powder which is freely soluble in water. Lobeline has been sold, in tablet form, for use as a smoking cessation aid, and may have application in the treatment of other drug addictions such as addiction to amphetamines, cocaine, or alcohol. Lobeline has multiple mechanisms of action, acting as a VMAT2 ligand, which stimulates dopamine release to a moderate extent when administered alone, but reduces the dopamine release caused by methamphetamine. It also inhibits the reuptake of dopamine and serotonin and acts as a mixed agonist-antagonist at nicotinic acetylcholine receptors to which it binds at the subunit interfaces of the extracellular domain. It is also an antagonist at μ-opioid receptors. It seems to be a P-glycoprotein inhibitor, according to at least one study. It has been hypothesized that P-glycoprotein inhibition reduces chemotherapeutic resistance in cancer, presumably affecting any substrates of P-gp.
Status:
Possibly Marketed Outside US
Source:
NCT04126135: Phase 4 Interventional Completed Nicotine Addiction
(2022)
Source URL:
First approved in 2018
Source:
Bei Ling Tong Bao Er Zheng Yuan Antibacterial Creams by Jilin Mancaotang Health Management Group Co Ltd
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Cytisine ( aka baptitoxine and sophorine) is a naturally occurring alkaloid that can be found in several plant genera, such as Laburnum and Cytisus of the family Fabaceae. It has been found to be clinically superior to nicotine replacement therapy for the cessation of smoking. It is available in Eastern Europe under the brand names Tabex and Desmoxan and in Canada under the brand name Cravv. However certain undesirable side effects exist, Cytisine can interfere with breathing and cause death (LD50 i.v., in mice, is about 2 mg/kg) and Cytisine is also teratogenic. Cytosine is an α4β2 nicotinic Acetylcholine receptor agonist. In addition to clinical use as a smoking cessation aid, It has demonstrated anti-depressant effects in mice.
Status:
Possibly Marketed Outside US
First approved in 2017
Source:
21 CFR 348
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Trimethylamine (or TMA) a tertiary amine, is synthesized by the action of microbial enzymes in humans. The decrease of TMA metabolism and excessive TMA excretion cause the disease trimethylaminuria and some other diseases associated with the abnormal level of TMA, e.g., obesity, diabetes, cardiovascular diseases. It was shown, that TMS is a full agonist of human trace amine-associated receptor 5, TAAR5. In addition, TMA is a precursor of N-oxide form, an emergent biomarker of human health that can lead to renal diseases, neurological disorders, and cancer.
Status:
Possibly Marketed Outside US
First approved in 2010
Source:
NADA092444
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Morantel (1,4,5,6-tetrahydro-1-methyl-2-[2-(3-methyl-2-thienyl)ethenyl pyrimidine) is a
tetrahydro-pyrimidine anthelmintic, differing from the related analogue pyrantel by the presence
of a methyl group on the thiophene ring. Morantel tartrate, manufactured by Pfizer, Inc., was approved in the United
States for use in cattle in 1981, and entered the market in early 1982. Three
formulations have been approved in the United States: RUMATEL®
Medicated Premix-88; RUMATEL Cattle Wormer Bolus, and PARATECT
FLEX™ Diffuser, a sustained release bolus. It is intended to treat roundworms and tapeworms. Morantel is
administered in lactating and non lactating cattle as morantel tartrate as a slow-release bolus
(11.8 g morantel base per animal) or as a single oral dose of 6 to 7.5 mg morantel base/kg bw and
in pigs at a single dose equivalent to 7.5 mg base/kg bw. In sheep, the citrate salt is administered
at a single dose equivalent to 5 to 6 mg morantel base/kg bw. Morantel acts as a potent agonist at the acetylcholine receptors on the muscle cells of nematodes.
Activation of the acetylcholine receptors induces a prolonged, spastic paralysis of the worms and
expulsion from the host. It also been reported to block neurotransmission in vertebrates, to
possess nicotine-like properties and to mimic acetylcholine at receptors in autonomic ganglia,
adrenal medullae and respiratory tissues. Morantel and its salts are not used in human medicines.
