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Restrict the search for
acetylcholine
to a specific field?
Status:
US Approved OTC
Source:
21 CFR 341.12(h) cough/cold:antihistamine doxylamine succinate
Source URL:
First approved in 1948
Source:
DECAPRYN by SANOFI AVENTIS US
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Doxylamine is an antihistamine commonly used as a sleep aid. This drug is also used to relieve symptoms of hay fever (allergic rhinitis), hives (rash or itching), and other allergic reactions. Doxylamine is a member of the ethanolamine class of antihistamines and has anti-allergy power far superior to virtually every other antihistamine on the market, with the exception of diphenhydramine (Benadryl). It is also the most powerful over-the-counter sedative available in the United States, and more sedating than many prescription hypnotics. In a study, it was found to be superior to even the barbiturate, phenobarbital for use as a sedative. Doxylamine is also a potent anticholinergic. Like other antihistamines, doxylamine acts by competitively inhibiting histamine at H1 receptors. It also has substantial sedative and anticholinergic effects. Used alone as a short-term sleep aid, in combination with other drugs as a night-time cold and allergy relief drug. Also used in combination with Vitamin B6 (pyridoxine) to prevent morning sickness in pregnant women.
Status:
US Approved OTC
Source:
21 CFR 336.10(c) antiemetic diphenhydramine hydrochloride
Source URL:
First approved in 1946
Source:
BENADRYL by MCNEIL CONS
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Diphenhydramine is an antihistamine which is used in the combination with naproxen sodium for the relief of occasional sleeplessness when associated with minor aches and pains. Diphenhydramine has a role nighttime sleep-aid and naproxen sodium is a pain reliever. In addition, diphenhydramine used in relieving symptoms in patients with moderate-to-severe seasonal allergic rhinitis. Diphenhydramine acts as an antagonist of histamine H1 receptor. Besides, was shown potential to repurpose diphenhydramine as an anti-melanoma therapeutic agent, it induces melanoma cell apoptosis by suppressing STAT3/MCL-1 survival signaling pathway.
Status:
Investigational
Source:
INN:aroxybutynin [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Investigational
Source:
INN:sofinicline [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Sofinicline is a selective agonist of the a4b2 subtype of nAChR. It is under development by Abbott Laboratories in collaboration with NeuroSearch. It is produced as a capsule in doses of 1, 2 or 4 mg. Sofinicline is a full agonist of the a4b2 nAChR. It has high
binding affinity, ~ 0.1 nM, for this receptor. Sofinicline is orally active and is metabolized hepatically. Sofinicline has been used in trials studying the treatment of ADHD, neuralgia, diabetic neuropathies, diabetic polyneuropathy, and diabetic neuropathic pain, among others.
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Xanomeline (LY-246,708) is an orthosteric muscarinic acetylcholine receptor (mAChR) agonist, often referred to as M1/M4-preferring. It is also known to act as a M5 receptor antagonist. Xanomeline was studied in clinical trials phase I in schizophrenia. In Phase II clinical trials in Alzheimer’s patients, xanomeline significantly improved several measures of cognitive function, yet produced unwanted side effects that limited patient compliance. The side effects seem to be associated with rapid metabolism of the alkyloxy side chain following oral administration, resulting in a nonselective, yet active compound with limited therapeutic utility. Despite a second Phase II clinical trial with a patch formulation, the liabilities of xanomeline still outweigh its benefits.
Status:
Investigational
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Meletimide (R 5183) is a powerful anticholinergic
agent with pronounced peripheral and central action.
Status:
Investigational
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Atropine-N-oxide hydrochloride is an alkaloid of the belladonna plants. It is the major metabolite of atropine. It is a competitive nonselective antagonist at central and peripheral muscarinic acetylcholine receptors.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Altinicline (SIB-1508Y, SIB-1765F) is a drug which acts as an agonist at neural nicotinic acetylcholine receptors with high selectivity for the α4β2 subtype. It stimulates release of dopamine and acetylcholine in the brain in both rodent and primate models, and progressed as far as Phase II clinical trials for Parkinson's disease, where "no antiparkinsonian or cognitive-enhancing effects were demonstrated", although its current status is unclear.
Status:
Investigational
Source:
INN:pozanicline [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Pozanicline is an alpha4-beta2 neuronal nicotinic receptor partial agonist. It had been in phase II clinical trials for the treatment of attention hyperactivity disorder and Alzheimer’s disease. It was tested for the treatment of schizophrenia too. All these studies were discontinued. Modulation of hippocampal learning and memory using Pozanicline in animal model was effective as novel therapeutic strategies for nicotine addiction. However future clinical trial was terminated.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Revatropate is a muscarinic antagonist with selectivity for M1 and M3 receptor subtypes. Significant improvement in airway function was shown in horses with heaves after inhalation of revatropate, and it was found to be a safe and effective bronchodilator. Early clinical studies in chronic obstructive airway disease (COAD) patients also showed that inhaled revatropate was an effective bronchodilator, and well tolerated.
