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hit2lead.com, Nicotinic agonists

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CYTISINE (485-35-8)  
Tsitizin  ·  cytisine hydrochloride, hydrate  ·  cytisine hydrochloride
Cytisine, also known as baptitoxine and sophorine, is an alkaloid that occurs naturally in several plant genera, such as Laburnum and Cytisus of the family Fabaceae. It has been used medically to help with smoking cessation. Its molecular structure has some similarity to that of nicotine and it has similar pharmacological effects.

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Xanthinol nicotinate (437-74-1)  
Xantinol Nicotinate  ·  Xanthinol Niacinate  ·  Xavin
Xanthinol is a drug prepared from theophylline used as a vasodilator. It is most often used as the salt with niacin (nicotinic acid), known as xantinol nicotinate.
Nikethamide (59-26-7)  
Coramine  ·  Coramin  ·  Cordiamine
Nikethamide is a stimulant which mainly affects the respiratory cycle. Widely known by its former trade name of Coramine, it was used in the mid-twentieth century as a medical countermeasure against tranquilizer overdoses, before the advent of endotracheal intubation and positive-pressure lung expansion. It is no longer commonly considered to be of value for such purposes.
XANOMELINE (131986-45-3)  
Xanomeline (LY-246,708; Lumeron, Memcor) is a muscarinic acetylcholine receptor agonist with reasonable selectivity for the M1 and M4 subtypes, though it is also known to act as a M5 receptor antagonist. It has been studied for the treatment of both Alzheimer's disease and schizophrenia, particularly the cognitive and negative symptoms, although gastrointestinal side effects led to a high drop-out rate in clinical trials. Despite this, xanomeline has been shown to have reasonable efficacy for the treatment of schizophrenia symptoms, and one recent human study found robust improvements in verbal learning and short-term memory associated with xanomeline treatment.
N-Benzylnicotinamide (2503-55-1)  
nicotinic acid benzylamide
(+/-)-Epibatidine (140111-52-0)  
Epibatidine is a putative alkaloid that is secreted by the Ecuadoran frog Epipedobates anthonyi. It was discovered by John W. Daly in 1974, but its structure was not fully elucidated until 1992.
Acetylcholine perchlorate (927-86-6)  
Acetylcholine  ·  Acetylcholine Chloride  ·  Miochol
N-Phenylnicotinamide (1752-96-1)  
nicotinanilide  ·  nicotinanilide monohydrochloride
CYTISINE (485-35-8)  
Tsitizin  ·  cytisine hydrochloride, hydrate  ·  cytisine hydrochloride
Cytisine, also known as baptitoxine and sophorine, is an alkaloid that occurs naturally in several plant genera, such as Laburnum and Cytisus of the family Fabaceae. It has been used medically to help with smoking cessation. Its molecular structure has some similarity to that of nicotine and it has similar pharmacological effects.
isoguvacine (64603-90-3)  
isoguvacine hydrochloride  ·  isoguvacine hydrobromide
Isoguvacine is a GABAA receptor agonist used in scientific research.
CGP-20712A (137888-49-4)  
2-hydroxy-5-(2-(hydroxy-3-(4-((1-methyl-4-trifluoromethyl)-1H-imidazol-2-yl)phenoxy)propyl)aminoethoxy)benzamide  ·  CGP-20712  ·  CGP 20712A
acetylcholine (51-84-3)  
Acetylcholine Chloride  ·  Miochol  ·  Acetylcholine Bromide
Acetylcholine (ACh) is an organic chemical that functions in the brain and body of many types of animals, including humans, as a neurotransmitter—a chemical released by nerve cells to send signals to other cells. Its name is derived from its chemical structure: it is an ester of acetic acid and choline. Parts in the body that use or are affected by acetylcholine are referred to as cholinergic.
Ifenprodil (23210-56-2, 23210-58-4)  
4-benzyl-alpha-(p-hydroxyphenyl)-beta-methyl-1-piperidineethanol  ·  ifenprodil tartrate (2:1), (R-(R*,R*))-isomer  ·  ifenprodil, (R*,S*)-(+-)-isomer
Ifenprodil is an inhibitor of the NMDA receptor, specifically of GluN1 (glycine-binding NMDA receptor subunit 1) and GluN2B (glutamate-binding NMDA receptor subunit 2) subunits. Additionally, ifenprodil inhibits GIRK channels, and interacts with alpha1 adrenergic, serotonin, and sigma receptors. NMDA receptors are multimeric ionotropic glutamate receptors composed of four subunits.
mecamylamine (60-40-2, 826-39-1)  
Mecamylamine (INN, BAN; or mecamylamine hydrochloride (USAN); brand names Inversine, Vecamyl) is a non-selective, non-competitive antagonist of the nicotinic acetylcholine receptors (nAChRs) that was introduced in the 1950s as an antihypertensive drug. In the United States, it was voluntarily withdrawn from the market in 2009 but was brought to market in 2013 as Vecamyl and eventually was marketed by Turing Pharmaceuticals. Chemically, mecamylamine is a secondary aliphatic amine, with a pKaH of 11.2
Gyki-52466 (102771-26-6)  
GYKI 52466  ·  1-(p-aminophenyl)-4-methyl-7,8-methylenedioxy-5H-2,3-benzodiazepine hydrochloride
GYKI-52466 is a 2,3-benzodiazepine that acts as an ionotropic glutamate receptor antagonist, which is a non-competitive AMPA receptor antagonist (IC50 values are 10-20, ~ 450 and >> 50 μM for AMPA- , kainate- and NMDA-induced responses respectively), orally-active anticonvulsant, and skeletal muscle relaxant. Unlike conventional 1,4-benzodiazepines, GYKI-52466 and related 2,3-benzodiazepines do not act on GABAA receptors. Like other AMPA receptor antagonists, GYKI-52466 has anticonvulsant and neuroprotective properties.
cirazoline (59939-16-1)  
LD-3098  ·  cirazoline monohydrochloride  ·  2-(2'-cyclopropylphenoxymethyl)imidazoline hydrochloride
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. Cirazoline has also been shown to decrease food intake in rats, purportedly through activation of α1 adrenoceptors in the paraventricular nucleus in the hypothalamus of the brain.
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