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Restrict the search for
acetylcholine
to a specific field?
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:
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
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 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.
Status:
Possibly Marketed Outside US
First approved in 2010
Source:
NADA092444
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
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.
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.
Status:
Possibly Marketed Outside US
Source:
NCT01842932: Phase 4 Interventional Unknown status Colonoscopy
(2009)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Cimetropium bromide (cimetropium) is a semi-synthetic belladonna alkaliod, a quaternary
derivatives of scopolamine. Cimetropium was used in Italy under the name Alginor for the treatment of painful gastrointestinal conditions, such as irritant bowel syndrome or infant colics as well as in preparation for diagnostic procedures. The drug exerts its action by binding to muscarinic receptors and inhibiting their activity.
Status:
Possibly Marketed Outside US
Source:
CERVOXAN
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Vinburnine is a nutritional product, a peripheral vasodilator with cerebral activities that also act as a cerebral metabolic stimulant and appears to be able to relax the smooth muscle cells within the walls of blood vessels. (+/-)-Eburnamonine is the racemate of the alkaloid Vinburnine. Dextrorotatory, levorotatory, and racemic forms of eburnamonine exist in nature. The (-)-form, also known as vincamone (isolated from Vinca minor), is a drug that possesses a stimulating activity for muscle and is used as cerebrotonic, whereas both enantiomers have hypotensive effects.
