fp receptor

L 888607 is an effective and selective CRTH2 agonist (Ki: 0.8 nM).

AZD5462 是一种有效可口服的松弛素受体 RXFP1 激动剂，可用于研究心力衰竭和癌症。

Latanoprost acid 是前列腺素受体的选择性激动剂，通过抑制 c-fos NFATc1 通路抑制 RANKL 诱导的破骨细胞生成和功能。 拉坦前列素酸可用于降低眼内压力的研究。

Bimatoprost acid (17-phenyl trinor PGF2α) 是一种代谢稳定的 PGF2α 类似物，对 FP 受体具有潜在的拮抗活性。与 PGF2α 相比，它与绵羊黄体细胞上的 FP 受体结合的相对效力为 756%。

Latanoprost (Xalatan) 是前列腺素 F2α 类似物，是一种前列腺素受体激动剂，能够降低眼内压。

Omidenepag isopropyl (DE-117) 是一种选择性前列腺素 EP2 受体激动剂，是一种新型局部眼部降低血压的化合物。Omidenepag isopropyl 对 EP1，EP2 和 FP 受体有弱亲和力。Omidenepag isopropyl 可用于研究青光眼和高眼压症。

BAY-6672是一种选择性的人前列腺素F（FP）受体拮抗剂，具有高效（IC50=11 nM），可口服和渗透性好的特点。通过拮抗FP受体抑制前列腺素F2α(PGF₂α)的活性，从而发挥抗纤维化作用，对动物模型的特发性肺纤维化（IPF）的具有体内疗效。

ONO-AE3-208 (AE 3-208) 是一种 EP4 拮抗剂，可抑制前列腺癌的细胞迁移、侵袭和转移。

Latanoprost lactone diol is an important intermediate compound in the synthesis of Latanoprost. Latanoprost, classified as a prostaglandin F2α analogue, functions as an agonist for the FP prostanoid receptor, resulting in a reduction in intraocular pressure (IOP).

RIP2 kinase inhibitor 1 is a potent and selective receptor interacting inhibitor of protein 2 (RIP2) kinase(RIP2 FP with an IC50 of 0.03 μM ),and is used for autoinflammatory disorders.

CAY10509 是一种 PGF2α 类似物，也是 FP 受体抑制剂，IC50 为 30 nM。有望用于研究前列腺素相关生理调节机制。

Latanoprosttris(triethylsilyl) ether 是 Latanoprost 合成的前体，它是前列腺素 F2α (PGF2α) 受体 (FP受体) 激动剂。

AL-8810 是 PGF2α的一种 11β- 氟类似物，对PGF2α受体(FP 受体) 具有选择性拮抗作用。

AS604872 is a selective antagonist of the FP receptor.. AS604872 significantly accelerated degeneration of the media in both cerebral artery and aorta as evidenced by thinning of the media and disruption of the elastic lamina and promoted IA and aortic di

(+) - cloprostenol sodium is a kind of water-soluble prostaglandin F2 α ( PGF2 α) Analogues. It is an FP receptor agonist and a potent luteinizing agent in rats and hamsters.

AL-3138 is a prostaglandin F2alpha (PGF2alpha) analogue which antagonizes FP prostanoid receptor-mediated inositol phosphates generation.

Latanoprost is an F-series prostaglandin (PG) analog which has been approved for use as an ocular hypotensive drug. Latanoprost is an isopropyl ester, a prodrug form which is converted to latanoprost (free acid) by endogenous esterase enzymes. The free acid form is 200 times more potent than latanoprost as a ligand for the human recombinant FP receptor. 5-trans Latanoprost (free acid) is an isomer of latanoprost (free acid) wherein the double bond between carbons 5 and 6 has been changed from cis (Z) to trans (E). The trans isomer of latanoprost occurs as an impurity in commercial preparations of the bulk drug product. The present compound was prepared primarily as an analytical standard for detection and quantitation of this impurity. From what can be inferred from the study of other trans isomers of F-type prostaglandins, the biological activity of this isomer is likely to be similar to that of the cis isomer. However, there are no specific published reports on the biological activity, and on reducing intraocular pressure in particular, of 5-trans latanoprost.

(+)-Cloprostenol is a synthetic analog of prostaglandin F2α (PGF2α). It is an FP receptor agonist and a potent luteolytic agent in rats and hamsters. It is 200 times and 100 times more potent than PGF2α in terminating pregnancy in hamsters and rats, respectively, without the side effects associated with PGF2α. Cloprostenol is also used in veterinary medicine as a luteolytic agent for the induction of estrus and the treatment of reproductive disorders in cattle, swine, and horses. (+)-Cloprostenol methyl ester is a more lipid soluble form of cloprostenol, which may be more amenable for certain formulations.

There are currently four prostaglandin (PG) derivatives which have been approved for human clinical use for the treatment of glaucoma. The names of the PGs and the concentrations of the approved doses are: travoprost (40 μg/ml), latanoprost (50 μg/ml), bimatoprost (300 μg/ml), and unoprostone (1,500 μg/ml). All of these compounds are modified at C-1 in order to act as lipophilic prodrugs in the eye. All have also been postulated to function via activation of the prostanoid FP receptor. Unoprostone and bimatoprost stand out in this class due to their lack of potency. Both are also claimed to have alternate mechanisms of actions: as a docosanoid in the case of unoprostone and as a prostamide in the case of bimatoprost. Lumula is a hybrid eicosanoid analog which incorporates the docosanoid features of unoprostone as well as the prostamide features of bimatoprost. Based on classical structure-activity relationships which have been established for prostanoid receptors

Prostaglandin F2α (PGF2α), acting through the FP receptor, causes smooth muscle contraction and exhibits potent luteolytic activity. 17-trifluoromethylphenyl trinor Prostaglandin F2α (17-trifluoromethylphenyl trinor PGF2α) is an analog of PGF2α that shares the meta-trifluoromethyl group of travoprost with the 17-phenyl trinor modification of latanoprost. It is anticipated to be a potent and selective agonist of the FP receptor, with potential applications in glaucoma and luteolysis. 17-trifluoromethylphenyl trinor PGF2α ethyl amide is a lipophilic analog of 17-trifluoromethylphenyl trinor PGF2α. Ethyl amides of PGs can serve as prodrugs, as they are hydrolyzed in certain tissues to generate the bioactive free acid.

Prostaglandin F1α (PGF1α) is the putative metabolite of dihomo-γ-linolenic acid (DGLA) via the cyclooxygenase (COX) pathway. Both PGF1α and PGF2α have been shown to act as priming pheromones for male Atlantic salmon with a threshold concentration of 10-11 M. [1] PGF1α binds to the ovine corpus luteum FP receptor at only 8% of the relative potency of PGF2α. [2] It is only half as active as PGF2α in inducing human respiratory smooth muscle contractions in vitro. [3]

17-phenyl trinor Prostaglandin F2α N-ethyl amide (17-phenyl trinor PGF2α) is an F-series prostaglandin analog which has been approved for use as an ocular hypotensive drug, sold under the Allergan trade name 17-phenyl trinor PGF2α ethyl amide. Investigations in our lab have shown that 17-phenyl trinor PGF2α ethyl amide is converted by an amidase enzymatic activity in the human cornea to yield the corresponding free acid, with a conversion rate of about 25 μg cornea 24 hours. The free acid, 17-phenyl trinor PGF2α, is a potent FP receptor agonist. 15(R)-17-phenyl trinor PGF2α is the 15-epi, or unnatural isomer of this active free acid metabolite. It has much diminished FP receptor-mediated activity

15(S)-Latanoprost is an analog of latanoprost in which the hydroxyl at carbon 15 is inverted relative to latanoprost. The IC50 values for the free acid forms of latanoprost and 15(S)-latanoprost were determined to be 3.6 nM and 24 nM, respectively, in a FP receptor binding assay using the cat iris sphincter muscle. A 3 μg dose of 15(S)-latanoprost caused a 1 mmHg reduction of IOP in normotensive cynomolgus monkeys. 15(S)-Latanoprost is a potential impurity in most commercial preparations of the latanoprost bulk drug product.

The actions of many clinical F-series prostaglandins (PGs), including those used for estrous synchronization and for reduction of intraocular pressure (IOP), are mediated through the PGF2α (FP) receptor. 16-phenoxy tetranor Prostaglandin F2α cyclopropyl methyl amide (16-phenoxy tetranor PGF2α cyclopropyl methyl amide) is an analog of PGF2α containing a 16-phenoxy group on the lower (ω) side chain and a cyclopropyl methyl amide at the C-1 position. There are no published reports on the biological activity of 16-phenoxy tetranor PGF2α cyclopropyl methyl amide.