Beta2-adrenergic agonist | Alpha-adrenergic agonist | The Agonist |
It is the first drug developed that is a highly selective agonist for the PD-168,077 and CP-226,269.
In biochemistry and pharmacology, an allosteric modulator is a substance which indirectly influences (modulates) the effects of an agonist or inverse agonist at a target protein, for example a receptor.
WAY-317,538 - selective potent full agonist with nootropic and neuroprotective properties
Antagonism (pharmacology), when a substance binds to the same site an agonist would bind to without causing activation of the receptor
It is an agonist of the opioid receptors, with evidence suggesting it serves as the endogenous ligand of the μ-opioid receptor, the same receptor to which the chemicals extracted from opium, such as morphine, have their analgesic and addictive effects (indeed, the μ-opioid receptor was named based on its most renowned ligand, morphine).
-{BRL-54443}-, agonist of 5-HT1E and 5-HT1F serotonin receptors
Binospirone, a partial agonist at 5HT1A somatodendritic autoreceptors
A-77636, a selective dopamine receptor D1 agonist
In a study conducted by Jürg Gertsch et al. from the Swiss Federal Institute of Technology (ETH Zurich), beta-caryophyllene was shown to be selective agonist of cannabinoid receptor type-2 (antiinflammatory effects in mice.
Scientists at Chugai discovered an erythromycin-derived motilin agonist called Mitemcinal (aka GM-611 or 3'-N-dimethyl-11-deoxy-3'-N-isopropyl-12-O-methyl-11-oxo-8,9-didehydroerythromycin.) Mitemcinal was believed to have strong prokinetic properties, similar to its parent molecule, but lack antibiotic properties.
Activating CMKLR1 by an agonist mobilizes intracellular calcium and causes the activation of several other signaling cascades like the ERK1 and NF-κB.
sigma receptor agonist (Ki = 205 nM and 11,060 nM, respectively).
This energetically favorable position of the agonist makes it possible for additional binding of the ligand to other Ser in the binding site, along with additional anchoring between Phe in the pocket of the binding site and the indole of the agonist.
Betahistine is a weak Histamine1 agonist but a very strong Histamine3 antagonist that is used to treat vertigo.
The candidate is being developed with a Toll-like receptor 3 (TLR3) agonist adjuvant for multiple indications, including cervical intraepithelial neoplasia (also known as cervical dysplasia or CIN), genital warts, cervical cancer, and head and neck cancers.
Depending on when a Hh inhibiting compound is approved by the U.S. Food and Drug Administration (FDA), there may be a perceived need for one to be differentiated over another for marketing purposes, which could lead to different nomenclature (e.g., a Hhi or an agonist of Smo).
LY-156735 (TIK-301, PD-6735) is a melatonin MT1 and MT2 agonist which is under development for the treatment of insomnia and other sleep disorders.
N6-Cyclopentyladenosine (CPA) is a drug which acts as a selective adenosine receptor agonist.
Nventa is developing HspE7 in combination with the Toll-like receptor 3 (TLR3) agonist adjuvant Poly-ICLC for multiple indications, including Cervical Intraepithelial Neoplasia (also known as cervical dysplasia or CIN), Genital Warts, Cervical Cancer, and head and neck cancers.
Oxymetazoline is a selective alpha-1 agonist and partial alpha-2 agonist topical decongestant, used in the form of Oxymetazoline hydrochloride, in products such as Afrin, Dristan, Nasivin, Logicin, Vicks Sinex, Visine L.R., Sudafed OM, Zicam and SinuFrin.
It was demonstrated that pamoic acid has agonist activity for the orphan G protein-coupled receptor GPR35 by which it activates ERK and beta-arrestin2, and causes antinociceptive activity.
Meta-analyses indicate that calcium-channel blockers and an oxytocin antagonist can delay delivery by 2–7 days, and β2-agonist drugs delay by 48 hours but carry more side effects.
René Descartes (1596–1650) was one of the first to conceive a model of reciprocal innervation (in 1626) as the principle that provides for the control of agonist and antagonist muscles.
Ro4938581 is a nootropic drug invented in 2009 by a team working for Hoffmann-La Roche, which acts as a subtype-selective inverse agonist at the benzodiazepine binding site on the receptor.
Vabicaserin (SCA-136) is a selective 5-HT2C full agonist that was being investigated as an antidepressant and atypical antipsychotic and was later dropped by its developer, Wyeth.
It binds to the partial agonist effect at α2 likely to be responsible for the lack of anxiety produced by this drug when compared to older α5-preferring inverse agonists such as L-655,708.