Proteina G/GPCR

<p>5-HT2A receptor agonist-3 represents the highest selectivity for the human 5-HT2A receptor currently identified, exhibiting a K i of 2.5 nM.</p>

<p>L-796568: potent β3 agonist (EC50 = 3.6 nM), &gt;600-fold selectivity vs β1/β2, good oral bioavailability, long action.</p>

<p>11-Keto Fluprostenol, a potent analog of prostaglandin F2α (PGF2α), primarily interacts with the FP receptor. It is a structurally modified derivative of prostaglandin D2 (PGD2) designed to enhance its potency and extend its half-life. The compound is produced by oxidizing fluprostenol at the C-11 position, which results in 11-keto fluprostenol. This modification allows 11-keto Fluprostenol to exhibit moderate affinity for the CRTH2/DP2 receptor, though it shows negligible activity at the DP1 receptor, distinguishing its action from that of PGD2.</p>

Domesticine, (-)- is an antagonist of alpha-1D-adrenoceptor.

YM-543/ASP-543: Potent, selective SGLT2 inhibitor, reduces blood sugar and improves glucose tolerance in diabetic mice.

<p>KP496 is a selective, dual antagonist for Thromboxane A2 receptor and Leukotriene D4 receptor.</p>

PF-184563 is an effective and selective non-peptide antagonist of the V1a receptor with oral activity, suitable for studying Raynaud's disease dysmenorrhoea.

15(S)-Fluprostenol isopropyl ester, an isomer of the prostaglandin F2α analog, fluprostenol isopropyl ester, serves as a possible prodrug to 15(S)-fluprostenol. It has the potential to act as an agonist at FP receptors, albeit with lower potency compared to the 15(R) epimer and the FP receptor agonist, fluprostenol. Additionally, it may be present as a potential impurity in commercial formulations of fluprostenol isopropyl ester.

AC-099 hydrochloride is a full agonist of neuropeptide FF2 receptor NPFF2R and a partial agonist of neuropeptide FF1 receptor NPFF1R.

(2R,3S)-E1R, an enantiomer of E1R, is a sigma-1 receptor modulator for treating cognitive disorders.

8,12-iso-iPF2α-VI, an isoprostane, arises from non-enzymatic, free radical-induced peroxidation of membrane lipids. It is the predominant isoprostane formed during lipid peroxidation and serves as a biomarker for oxidative stress. Detectable in hepatic tissue post CCl4-induced oxidative damage, 8,12-iso-iPF2α-VI levels are also elevated in the urine, blood, and cerebrospinal fluid of Alzheimer's disease patients.

17-Phenyl trinor Prostaglandin F2αdiethyl amide (17-phenyl trinor PGF2αdiethyl amide) is a Prostaglandin F2α(PGF2α) analog characterized by the substitution of the C-1 carboxyl group with an N-diethyl amide. Prostaglandin (PG) esters and N-ethyl amides have demonstrated ocular hypotensive properties, with N-ethyl amides introduced as alternative options for PG hypotensive prodrugs. Studies indicate that both bovine and human corneal tissues can convert N-ethyl amides of various PGs into their free acid forms at a rate of approximately 2.5 µg/g corneal tissue/hr. However, dialkyl amides like 17-phenyl trinor PGF2αdiethyl amide resist conversion by corneal amidase, showing no detectable transformation into free acids. This characteristic suggests their potential as valuable investigative tools for assessing the intrinsic intraocular hypotensive activities of PG amides.

Ubrogepant (MK-1602) is an antagonist of calcitonin gene-related peptide receptor that can be used in the acute treatment of migraine studies.

<p>CP-122288: potent, selective 5-HT1B/D/F agonist; inhibits plasma protein extravasation, neurogenic inflammation.</p>

SDZ-NVI-085 is an α1 adrenergic receptor agonist and a competitive antagonist of 5-hydroxytryptamine.

GSK-1004723 is a novel antagonist of histamine H(1) and H(3) receptor. It represents a potential novel therapy for allergic rhinitis.

TA-1887: Selective SGLT2 inhibitor, treats type 2 diabetes, lowers glucose in high-fat diet mice, boosts UGE, has good pharmacokinetics.

Indacaterol xinafoate is an ultra-long-acting beta-adrenoceptor agonist.

Hemopressin(rat) TFA, a nonapeptide from hemoglobin α1-chain, selectively inhibits CB1 receptors and reduces inflammatory pain.

Prostaglandin F2α serinol amide, a serinolamide G protein-coupled receptor, elevates calcium levels in human non-small cell lung cancer cells. Additionally, Prostaglandin F2α functions as a luteinizing hormone in sheep and potentially serves as a nociceptive mediator in the spinal cord [1] [2] [3].