agonistic

Sorafenib (Bay 43-9006) is a multikinase inhibitor that targets Raf-1, B-Raf, VEGFR2, VEGFR3, VEGFR4, PDGFRβ, FLT3, c-Kit, and others (IC50=6 22 90 15 20 20 57 58 nM) with oral activity. It exhibits antitumor properties and can induce autophagy, apoptosis, and agonistic iron death.

1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(7-(1-methyl-1H-pyrazol-4-yl)-2,3,4,9-tetrahydro-1H-carbazol-3-yl)urea, a TNF-α agonistic compound, could induce cells to secrete TNF- α.

Viloxazine (Viloxazin) (Viloxazin) is a dual-action compound that functions as a norepinephrine reuptake inhibitor and exhibits potent agonistic activity towards 5-HT 2C receptors while acting as an antagonist for 5-HT 2B receptors, with respective potency values of EC 50 = 32 μM and IC 50 = 27 μM. Its primary mechanism of action involves the modulation of serotonergic and noradrenergic pathways. Viloxazine is commonly employed in depression research [1] [2].

Sorafenib tosylate (Bay 43-9006) is a potent multikinase inhibitor (IC50s: 6 20 22 nM for Raf-1 VEGFR-3 B-Raf).

Carbachol (Carbamoylcholine chloride), an analog of acetylcholine, serves as a valuable tool in the investigation of various physiological responses mediated by nicotinic (nAChR) and muscarinic (mAChR) acetylcholine receptors. These responses include smooth muscle contraction, gut motility, and neuronal signaling. Known for its agonistic properties, Carbachol activates both nAChR and mAChR, with reported Ki values ranging from 10 to 10,000 nM for different receptor types and experimental preparations.

Gliquidone (AR-DF 26) is a potent, second-generation sulfonylurea with antihyperglycemic activity, exhibiting greater binding affinity to SUR1 and increased potency compared to first-generation compounds. Additionally, this agent exerts peroxisome proliferator-activated receptor (PPAR) gamma agonistic activity.

NSC-5844 (RE-640) (RE640) is a bisquinoline compound with C-C chemokine receptor type 1 (CCR1)-agonistic activities.

FLTX1 is a fluorescent derivative of Tamoxifen, designed to efficiently target and label intracellular Tamoxifen-binding sites (estrogen receptors) both under permeabilized and non-permeabilized conditions. Additionally, FLTX1 demonstrates strong antiestrogenic activity in breast cancer cells, resembling the potent antiestrogenic properties of Tamoxifen. Notably, FLTX1 does not exhibit any estrogenic agonistic effect on the uterus.

L-Cysteinesulfinic acid is an endogenous neurotransmitter with agonistic effects on a variety of metabotropic glutamate receptors (mGluRs), including mGluR1, mGluR5, mGluR2, mGluR4, mGluR6, and mGluR8, with a pEC50 = 2.7 to 4.0. L- Cysteinesulfinic acid is a pld-coupled agonist of metabotropic excitatory amino acid (EAA) receptors.

(+)-Cloprostenol is a analogue of prostaglandin F2α (PGF2α), and is selective prostaglandin receptor agonistic.

Axomadol (EN3324) is a centrally active analgesic compound with opioid agonistic properties and inhibitory effects on the reuptake of monoamines.

Etofylline clofibrate has a hypolipidemic and antithrombotic effect and it also has an agonistic interaction with intimal PGI2.

ZK159222 is an effective 1α,25-(OH)2D3 receptor (VDR) agonist. ZK159222 has a partial agonistic character.

TAAR1 agonist 2 (compound 30), a full agonist at trace amine-associated receptor 1 (TAAR1) (pEC50=7.5), also displays agonistic properties at H1 receptors and activates various muscarinic acetylcholine receptors, including the M2 receptor (pEC50=5). This compound is utilized in researching neuropsychiatric diseases.

LBG20304 (compound 2s) serves as a ligand for the homologous GluK5 receptor, demonstrating an IC50 of 432 nM and exhibiting over 40-fold selectivity against the GluK1-3 isoforms. At concentrations below 10 μM, LBG20304 shows neither agonistic nor antagonistic effects on heterologous GluK2 5 receptors. However, at concentrations above 10 μM, it displays minimal agonist activity in neuronal slices (rat).

TLR7 agonist27 (compound 24) is an effective TLR7 agonist with an EC50 of 238.1 nM. It exhibits weak agonistic activity towards NOD2 (nucleotide-binding oligomerization domain 2) with an EC50 of 6.2 μM. TLR7 agonist27 serves as a potent immunostimulant and can be utilized as a vaccine adjuvant and or an immunotherapeutic agent.

TAS-108 (also known as SR-16234) is a selective estrogen receptor modulator (SERM) reported to exhibit antagonistic activity towards estrogen receptor (ER) α, while demonstrating high affinity and weak partial agonistic activity for the ERβ receptor.

RU-16117, an 11 alpha-methoxy derivative of ethynyl estradiol, is an orally active weak estrogen that might be effective in treating estrogen deficiencies in postmenopausal women. This compound exhibits partial estrogen agonistic antagonistic properties. RU-16117 can inhibit basal gonadotropin secretion and diminish the LH response to LHRH.

Ritobegron (also known as KUC-7483) is a potent and selective β3-adrenergic receptor agonist. In studies involving transfected human β-AR, Ritobegron exhibits significant and selective agonistic activity towards β(3)-AR. In rats, it shows high selectivity for the bladder over other organs. In anesthetized rats, Ritobegron effectively reduces bladder pressure with minimal impact on the cardiovascular system. It holds potential as a compound for treating overactive bladder.

4,8-Dioxa-3H-perfluorononanoic acid, a type of per- and polyfluoroalkyl substance (PFAS), exhibits affinity for the human pregnane X receptor (hPXR) and demonstrates potential agonistic activity.

KOR agonist 5 (Compound 10a) is both a KOR MOR modulator, exhibiting agonistic effects on KOR and antagonistic effects on MOR. It effectively blocks morphine-induced antinociception and gastrointestinal motility inhibition. KOR agonist 5 is applicable in research related to substance use disorder (SUD).

Inactive analog of m-3M3FBS (PLC activator)

The substitution with Sar at position 1 of angiotensin II resulted in a partial agonistic activity.

Onzigolide (BIM-23A760), a chimeric compound with properties of both dopamine and somatostatin, exhibits strong agonistic activity towards dopamine D2 receptors (D2R) and somatostatin type 2 receptors (SSTR2).