FP receptor; prostaglandin F (PGF) receptor; Endogenous Metabolite

当山羊黄体细胞暴露于地诺前列素（前列腺素 F2α；1 μM）一整天时，会发生坏死、自噬和内质网脱垂 [1]。地诺前列素 (1 μM) 在 24 小时内显着升高 GRP78 和 UPR 传感器。

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PGF2α（10（-6）M）和氟前列醇（10（-6M）M）抑制了ET-1诱导的离体BTM（10（-8）M）收缩。这种作用被FP受体拮抗剂阻断。卡巴胆碱诱导的收缩或基线张力不受PGF2alpha或氟前列醇的影响。在培养的TM细胞中，ET-1导致[Ca2+]i短暂增加，而PGF2α会降低[Ca2+]i。在FP受体拮抗剂Al-8810存在的情况下没有发生减少。Western blot分析揭示了FP受体在天然和培养的TM中的表达。 结论：FP受体激动剂通过与ET-1诱导的TM收缩性直接相互作用来发挥作用。这种作用是由FP受体介导的。因此，FP受体激动剂可以通过抑制ET-1依赖性机制来增强通过TM的房水流出，从而降低IOP。[1]

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黄体（CL）是一种短暂的内分泌组织，产生黄体酮以维持哺乳动物的妊娠。此外，CL的回归对于启动动情周期是必要的。广泛的研究表明，前列腺素F2α（PGF2α）诱导反刍动物CL的消退。然而，PGF2α诱导的山羊CL消退中内质网应激和自噬的机制尚不清楚。在这项研究中，收集了发情山羊和怀孕3个月的山羊的卵巢，以检测ER应激相关蛋白GRP78的位置。western blot分析证实了山羊CL在发情周期中黄体期不同阶段与ER应激相关蛋白和自噬相关蛋白表达变化之间的关系。结果表明，在山羊CL的黄体晚期，ER应激和自噬都被激活。为了揭示ER应激和自噬在PGF2α诱导的CL消退过程中的作用，我们分别使用4-苯基丁酸（4-PBA）和氯喹（CQ）抑制ER应激和自体吞噬。通过流式细胞术检测到的凋亡率和蛋白质印迹检测到的ER应激和自噬相关蛋白的表达，我们证明ER应激促进了山羊黄体细胞的凋亡和自噬，并且抑制自噬可以增强凋亡。此外，敲除阻断PERK通路激活的EIF2S1，通过减少PGF2α处理的山羊黄体细胞的自噬来促进凋亡。总之，我们的研究表明，内质网应激通过PERK信号通路促进山羊黄体细胞凋亡以调节CL的回归，并激活自噬以抑制山羊黄体细胞的凋亡[2]。

细胞凋亡分析 [1]
细胞类型： 山羊黄体细胞
测试浓度： 1 μM
孵育时间： 24 hrs（小时）
实验结果：细胞凋亡率显着增加（15.62±3.12%）。自噬检测 [1]
细胞类型： 山羊黄体细胞
测试浓度： 1 μM
孵育时间： 24 hrs（小时）
实验结果：黄体细胞中LC3和LAMP1存在广泛重叠，山羊黄体细胞中形成自噬溶酶体。

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蛋白质印迹分析[1]
细胞类型： 山羊黄体细胞
测试浓度： 1 μM
孵育持续时间：24小时
实验结果：GRP78和UPR传感器的表达，包括裂解的ATF6、磷酸-EIF2S1、EIF2S1、ATF4、磷酸-IRE1、自体吞噬作用相关胞内蛋白LC3-II和促凋亡因子cleaved Caspase3显着增加。

Goat ovaries were collected from sexually mature healthy goats and from goats that were pregnant for 3 months in a local abattoir within 10–20 min of slaughter. The duration of pregnancy was determined by the size and morphological characteristics of the fetus. Fresh ovaries stored on ice were taken back to our laboratory within 30 min for subsequent sampling. The complete CL was exfoliated during the estrous cycle from the non-pregnant goats’ ovaries on ice, and each CL was divided into two equal parts. These CL tissues were frozen in liquid nitrogen and stored at −80°C until RNA and protein extraction. Based on the detection of morphological characteristics and the levels of marker genes’ expression, such as STAR, 3βHSD, LH-R, and CYP19A1, in these goat CLs as previously described (Farin et al., 1986), the stages of the luteal phase of the CLs were categorized into five main groups [i.e., early (1–3 day after ovulation), mid1 (4–7 day after ovulation), mid2 (8–12 day after ovulation), mid3 (13–16 day post-ovulation), and late (17–20 post-ovulation)] (Figures 1B,C). For one independent experiment, we exfoliated goat CLs from at least three ovaries in each luteal stage (n = 3 ovaries per stage). All other ovaries fixed in paraformaldehyde (4%) for immunohistochemistry analysis were collected from three dioestrus goats and three pregnant goats.

Absorption, Distribution and Excretion
AMONG COMPD OCCURRING IN SEMEN THAT ARE OF CURRENT RESEARCH INTEREST ARE PROSTAGLANDINS (25 MG/ML). /PROSTAGLANDINS/
APART FROM GENERALLY SLOW & SPECIES-DEPENDENT ISOMERIZATION, PGS E & F ARE RATHER STABLE IN BLOOD, BUT THEY ARE RAPIDLY DEGRADED & INACTIVATED BY TISSUE-BOUND ENZYMES; SOME 80-90% OR MORE IS DESTROYED DURING SINGLE PASSAGE THROUGH LIVER OR LUNGS. /PROSTAGLANDINS/
DEG OF BINDING OF PROSTAGLANDINS TO PLASMA PROTEINS APPEARS TO HAVE LITTLE INFLUENCE ON THEIR RATES OF METABOLISM & ELIMINATION. ... CLEARANCE RATES OF (3)H DID NOT CHANGE WHETHER PROSTAGLANDINS WERE ADMIN IN FREE FORM OR BOUND TO RAT PLASMA ALBUMIN. /PROSTAGLANDINS/

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Metabolism / Metabolites
...PROSTAGLANDINS ARE RAPIDLY METABOLIZED... /PROSTAGLANDINS/

Interactions
CONTRACTIONS IN RESPONSE TO PROSTAGLANDIN F2ALPHA IN HUMAN ISOLATED BRONCHIAL MUSCLE ARE INHIBITED BY FENAMATES, PHENYLBUTAZONE, &, LESS POTENTLY, ASPIRIN.

[1]. Endothelin antagonism: effects of FP receptor agonists prostaglandin F2alpha and fluprostenol on trabecular meshwork contractility. Invest Ophthalmol Vis Sci. 2006 Mar;47(3):938-45.

[2]. Prostaglandin F2α Induces Goat Corpus Luteum Regression via Endoplasmic Reticulum Stress and Autophagy. Front Physiol. 2020 Sep 11;11:868.

Prostaglandin F2alpha is a prostaglandins Falpha that is prosta-5,13-dien-1-oic acid substituted by hydroxy groups at positions 9, 11 and 15. It is a naturally occurring prostaglandin used to induce labor. It has a role as a human metabolite and a mouse metabolite. It is a prostaglandins Falpha and a monocarboxylic acid. It is a conjugate acid of a prostaglandin F2alpha(1-).
Dinoprost has been investigated in Headache.
Dinoprost has been reported in Homo sapiens, Cervus nippon, and other organisms with data available.
Dinoprost is a synthetic analogue of the naturally occurring prostaglandin F2 alpha. Prostaglandin F2 alpha stimulates myometrial activity, relaxes the cervix, inhibits corpus luteal steroidogenesis, and induces luteolysis by direct action on the corpus luteum. (NCI04)
Prostaglandin F2alpha is a naturally occurring prostaglandin that stimulates myometrial activity, relaxes the cervix, inhibits corpus luteal steroidogenesis, and induces luteolysis by direct action on the corpus luteum. Expression of prostaglandin F2alpha (PGF2) is elevated in certain types of cancers.
A naturally occurring prostaglandin that has oxytocic, luteolytic, and abortifacient activities. Due to its vasocontractile properties, the compound has a variety of other biological actions.
See also: Dinoprost Tromethamine (has salt form).

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Mechanism of Action
...THERE IS NO SINGLE PROSTAGLANDIN RECEPTOR. ... IT IS POSSIBLE TO DEMONSTRATE CALCIUM DEPENDENCE OF DIVERSE RESPONSES TO PROSTAGLANDINS & TO OBSERVE ALTERED CALCIUM FLUXES. ...PROSTAGLANDINS MAY EITHER STIMULATE OR INHIBIT ACCUM OF CYCLIC AMP. /PROSTAGLANDINS/
RESPONSES TO PROSTAGLANDIN F2ALPHA SHOW SPECIES VARIATION, BUT VASODILATATION HAS BEEN OBSERVED FOLLOWING INJECTION INTO HUMAN BRACHIAL ARTERY OF PGF2ALPHA... SUPERFICIAL VEINS OF HAND ARE CONTRACTED BY PFG2ALPHA...
PROMPT SUBSIDENCE OF PROGESTERONE OUTPUT & REGRESSION OF CORPUS LUTEUM FOLLOWS PARENTERAL INJECTION OF PROSTAGLANDIN F2ALPHA... THIS EFFECT INTERRUPTS EARLY PREGNANCY, WHICH IS DEPENDENT ON LUTEAL RATHER THAN PLACENTAL PROGESTERONE.
OXYTOCIN & PROSTAGLANDINS AFFECT UTERINE SMOOTH MUSCLES BY DIFFERENT MECHANISMS, & THEIR EFFECTS ARE ADDITIVE. POSSIBLE ADVANTAGES OF THEIR COMBINED USE ARE BEING EXPLORED. /PROSTAGLANDINS/

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Therapeutic Uses
Abortifacient Agents, Nonsteroidal; Oxytocics
...SOME PHYSICIANS PREFER TO DEFER ABORTION UNTIL AFTER 16TH WK, WHEN INTRA-AMNIOTIC ROUTE CAN BE EMPLOYED MORE SAFELY. /DINOPROST TROMETHAMINE/
EXTRA-AMNIOTIC TECHNIQUE, WHICH IS STILL INVESTIGATIONAL, REQUIRES TRANSVAGINAL INTRAUTERINE EXTRAOVULAR PLACEMENT OF INDWELLING CATHETER. ... RESERVED FOR TERMINATION OF PREGNANCIES BETWEEN 13TH & 15TH WK... /DINOPROST TROMETHAMINE/
DOSAGE THAT ACHIEVES EFFECTIVE CONCN WITHIN MYOMETRIUM IS LOWEST WITH INTRAUTERINE ADMIN. INTRA-AMNIOTIC INSTILLATION IS ACCOMPLISHED WITH LONG SPINAL NEEDLE INSERTED TRANSABDOMINALLY INTO AMNIOTIC SAC. /DINOPROST TROMETHAMINE/
For more Therapeutic Uses (Complete) data for PROSTAGLANDIN F2ALPHA (15 total), please visit the HSDB record page.

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Drug Warnings
ASTHMATIC INDIVIDUALS ARE PARTICULARLY SENSITIVE, & PGF2ALPHA HAS CAUSED INTENSE BRONCHOSPASM.
SOME INVESTIGATORS HAVE INDICATED THAT PROSTAGLANDINS MAY SHOW NARROWER DOSE-RESPONSE RANGE FOR PRODN OF PHYSIOLOGICAL CONTRACTIONS & OCCURRENCE OF UTERINE HYPERTONUS, POTENTIAL HAZARD THAT MAY BE AVOIDED BY VERY CAUTIOUS STEPWISE INCREMENTS IN RATE OF INFUSION. /PROSTAGLANDINS/
FOR ABORTION IN 2ND TRIMESTER...RESULTS IN...FREQUENT BUT TOLERABLE SIDE EFFECTS. HOWEVER, FOR VERY EARLY ABORTION (MENSES DELAYED UP TO SEVERAL WK), RATE OF SUCCESS REPORTED IS LOW & SERIOUS SIDE EFFECTS HAVE RESULTED FROM DOSES REQUIRED. /PROSTAGLANDINS/
...CONTRAINDICATED IN ACUTE PELVIC INFLAMMATION. IT SHOULD BE USED CAUTIOUSLY IN PT WITH HISTORY OF HYPERTENSION, ASTHMA, GLAUCOMA, EPILEPSY, OR CARDIOVASCULAR DISEASE.
For more Drug Warnings (Complete) data for PROSTAGLANDIN F2ALPHA (11 total), please visit the HSDB record page.

C20H34O5

354.4810

354.24

C, 67.77; H, 9.67; O, 22.57

551-11-1

Dinoprost tromethamine salt;38562-01-5;(5R)-Dinoprost;4510-16-1;Dinoprost-d4;34210-11-2;Dinoprost-d9

5280363

White to light brown <25°C powder,>35°C liquid

1.2±0.1 g/cm3

531.0±50.0 °C at 760 mmHg

120°C

289.0±26.6 °C

0.0±3.2 mmHg at 25°C

1.569

2.14

97.99

4

5

12

25

432

5

O([H])[C@@]1([H])C([H])([H])[C@]([H])([C@]([H])(/C(/[H])=C(\[H])/[C@]([H])(C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H])O[H])[C@@]1([H])C([H])([H])/C(/[H])=C(/[H])\C([H])([H])C([H])([H])C([H])([H])C(=O)O[H])O[H]

PXGPLTODNUVGFL-YNNPMVKQSA-N

InChI=1S/C20H34O5/c1-2-3-6-9-15(21)12-13-17-16(18(22)14-19(17)23)10-7-4-5-8-11-20(24)25/h4,7,12-13,15-19,21-23H,2-3,5-6,8-11,14H2,1H3,(H,24,25)/b7-4-,13-12+/t15-,16+,17+,18-,19+/m0/s1

(Z)-7-((1R,2R,3R,5S)-3,5-dihydroxy-2-((S,E)-3-hydroxyoct-1-en-1-yl)cyclopentyl)hept-5-enoic acid

Cerviprost; HSDB 3315; Panacelan; Prostaglandin F2a; Prostaglandin F2alpha; Prostaglandin F2a; PGF2alpha; amoglandin; Enzaprost; Protamodin;

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

H2O : ~100 mg/mL (~282.10 mM)
DMSO : ~100 mg/mL (~282.10 mM)

配方 1 中的溶解度: ≥ 2.5 mg/mL (7.05 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 2.5 mg/mL (7.05 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。