Lasofoxifene Tartrate is a non-steroidal selective estrogen receptor modulator (SERM).
(-)-Penbutolol ((S)-Penbutolol) is a potent β-adrenoceptor and 5-HT receptor antagonist with Ki values of 11.6 nM and 11.9 nM for 5-HT in rat cornu ammonis 1 (CA1) and human CA3. (-)-Penbutolol can increase hippocampal 5-HT output[1][2].
Bis-propargyl-PEG9 is a PEG-based PROTAC linker used in the synthesis of PROTACs. Bis-propargyl-PEG9 can be used to synthesize the bivalent estrogen receptor ligands[1].
Norethisterone enanthate is a long-acting parenteral progestogen. Norethisterone enanthate is orally active[1][2][3].
Esomeprazole ((S)-Omeprazole) is a potent and orally active proton pump inhibitor and reduces acid secretion through inhibition of the H+, K+-ATPase in gastric parietal cells. Esomeprazole has the potential for symptomatic gastroesophageal reflux disease research[1][2][3].
Diethylstilbestrol, a synthetic nonsteroidal estrogen used in the treatment of menopausal and postmenopausal disorders.Target: Estrogen Receptor/ERRDiethylstilbestrol (DES), a synthetic estrogen that was used in pregnancy, is a prototype endocrine-disrupting chemical. Although prenatal exposure to DES is known to increase risks of vaginal/cervical adenocarcinoma and adverse reproductive outcomes in women, and urogenital anomalies in men, data on nonreproductive medical conditions are lacking. Comparing persons exposed prenatally to DES with those who were not exposed, the hazard ratios were 1.21 (95% confidence interval = 0.96-1.54) for diabetes, 1.27 (1.00-1.62) for all cardiovascular disease, 1.18 (0.88-1.59) for coronary artery disease, 1.28 (0.88-1.86) for myocardial infarction, 1.12 (1.02-1.22) for high cholesterol, 1.14 (1.02-1.28) for hypertension, 1.24 (0.99-1.54) for osteoporosis, and 1.30 (0.95-1.79) for fractures. The associations did not differ by dose and timing of DES exposure, nor, in the women, by the presence or absence of vaginal epithelial changes (a marker of DES host susceptibility) [1]. The role of prenatal exposure to DES as an environmental risk factor for psychiatric disorders requires more evidence before any conclusions can be drawn [2].
Methionyl-Lysyl-Bradykinin (Met-Lys-Bradykinin), a Bradykinin (HY-P0206) analogue, is a kinin[1][2].
Indacaterol-d3 is deuterium labeled Indacaterol.
FA-Ala-Arg is a dipeptide with furylacryloyl group. FA-Ala-Arg breaks down to produce arginine. While cell-surface Carboxypeptidase-D (CPD) also increases intracellular Arg, which is converted to nitric oxide (NO). FA-Ala-Arg enhances NO production in MCF-7 cells. FA-Ala-Arg also increases the cell survival of prolactin (PRL)-treated cells, PRL regulates CPD mRNA levels in cells[1].
Tibolone is a broad spectrum gonadal steroid agonist with progestagenic, androgenic, and estrogenic activities. Tibolone can be used for postmenopausal osteoporosis research[1][2].
Hydroxyzine D4 is deuterium labeled Hydroxyzine. Hydroxyzine is a heterocyclic histamine H1-receptor antagonist. Hydroxyzine has anticholinergic, anxiolytic and analgesic properties[1].
sGnRH-A is a salmon gonadotropin-releasing hormone (GnRH) analogue that stimulates growth hormone secretion and can also be used as an inducer of ovulation by artificial insemination[1][2].
Prostaglandin B2 is a prostaglandin. Prostaglandin B2 is the main substance in cord blood mesenchymal stem cells, to inhibit DC-T Cell proliferation. Prostaglandin B2 also induces cutaneous vasoconstriction of the canine hind paw[1][2].
SecinH3 is an antagonist of cytohesins with IC50s of 5.4 μM, 2.4 μM, 5.4 μM, 5.6 μM, 5.6 μM and 65 μM for hCyh1, hCyh2, mCyh3, hCyh3, drosophila steppke and yGea2-S7, respectively.
(±)-WB 4101 is a potent antagonist of noradrenaline. (±)-WB 4101 interacts with protein in smooth muscle. (±)-WB 4101 makes drug and receptor bind tightly[1].
3-Keto petromyzonol, a main component of Sea lamprey male sex pheromones, modulates both synthesis and release of gonadotropin releasing hormone (GnRH), and subsequently, hypothalamic-pituitary-gonadal (HPG) output in immature sea lamprey[1].
LY88074 (Compound 88074) is a Raloxifene analog lacking the basic side chain. Raloxifene is a selective estrogen receptor modulator, and reduces fracture risk at least in part by improving the mechanical properties of bone in a cell- and estrogen receptor-independent manner[1].
[Tyr0] Corticotropin Releasing Factor, ovine is a corticotropin releasing factor/hormone isolated from ovine. Corticotropin releasing factor (CRF) is a hypothalamic hormone, stimulates the release of adrenocorticotropic hormone (ACTH) and of β-endorphin[1][2].
LML134 (compound 18b) is an orally active and high selective Histamine 3 receptor (H3R) inverse agonist with Kis of 0.3 nM and 12 nM for hH3R cAMP and hH3R bdg. LML134 penetrates the brain rapidly, leading to high H3R occupancy, and disengages its target with a fast kinetic profile. LML134 is for the treatment of excessive sleep disorders[1].
pTH-Related Protein (1-40) (human, mouse, rat) stimulates calcium uptake in rat intestinal cells through PTHR1 receptor and PKCα/β signaling pathways. pTH-Related Protein (1-40) up-regulates parathyroid hormone 1 receptor (PTHR1) protein, four transcellular calcium transporters, potential vanillin member 6 (TRPV6), calcium-binding protein-D9K (CaBP-D9k), sodium-calcium Exchanger 1 (NCX1) and plasma membrane calcium ATPase 1 (PMCA1)[1].
Clenproperol-D7 is the deuterium labeled Clenproperol. Clenproperol is a β2-adrenergic agonist[1].
Tafluprost acid (AFP-172), an active metabolic form of Tafluprost, is a selective prostanoid FP receptor agonist. Tafluprost acid shows a high affinity for human prostanoid FP receptor with Ki and EC50 values of 0.4 nM and 0.53 nM, respectively. Tafluprost acid has 126 times weaker binding affinity for prostanoid EP3 receptor (IC50=67 nM) than for the prostanoid FP receptor. Tafluprost acid can be used in the research of glaucoma[1][2][3].
Olodaterol (BI1744) is a selective, long acting β2-adrenoceptor (β2-AR) agonist (EC50=0.1 nM and pKi= 9.14 for human β2-adrenoceptor, respectively). Olodaterol can be used for chronic obstructive pulmonary disease (COPD) and pulmonary fibrosis[1][2][3].
Gestodene(SHB 331;WL 70) is a progestogen hormonal contraceptive.Target: Estrogen Receptor/ERRGestodene is androgenically neutral, meaning that contraceptive pills containing gestodene do not exhibit the androgenic side effects (e.g. acne, hirsutism, weight gain) often associated with second-generation contraceptive pills, such as those containing levonorgestrel. When 40 micrograms of gestodene was taken, six out of seven women did not ovulate, and one out of seven had a cycle with luteal insufficiency. These data indicate that 40 micrograms of gestodene is the borderline dose for inhibition of ovulation. A combination of 75 micrograms gestodene with 30 micrograms ethinyl estradiol was found to inhibit ovulation in ten subjects, and no follicular maturation was noted [1]. gestodene bound with high affinity to the progesterone receptor, as did other synthetic and natural progestogens. However, gestodene did not bind to the estradiol receptor. The relative binding affinities of all tested synthetic and natural ligands showed no organ-specific differences and no differences between neoplastically transformed and normal tissues [2].Clinical indications: Female contraception
Veldoreotide (DG3173) a somatostatin analogue, that can bind to and activate the somatostatin receptors (SSTR) 2, 4, and 5. Veldoreotide inhibits growth hormone (GH) secretion in adenomas compared with Octreotide (HY-P0036). Veldoreotide has the potential to be used as pain modulating agent[1]
Proglumide hemicalcium is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide hemicalcium selective blocks CCK’s effects in the central nervous system (CNS). Proglumide hemicalcium has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide hemicalcium also has antiepileptic and antioxidant activities[1][2][3][4][5].
(d(CH2)51,Tyr(Me)2,Thr4,Orn8,des-Gly-NH29)-Vasotocin, an oxytocin receptor antagonist, abolishes oxytocin-enhanced inhibitory postsynaptic currents in CA1 pyramidal neurons[1].
Kisspeptin-54(human) (Metastin(human)) is an endogenous ligand for kisspeptin receptor (KISS1, GPR54). Kisspeptin-54(human) binds to rat and human GPR54 receptors with Ki values of 1.81 nM and 1.45 nM, respectively. Kisspeptin-54(human) hinders tumor metastasis and stimulates gonadotropin secretion[1][2].
Zaltidine(CP-57361) is a H2-receptor antagonist, which has the antisecretory action.IC50 Value: Target: H2 receptorin vitro:in vivo: In eight healthy male volunteers single oral doses of 5 mg, 25 mg and 100 mg produced dose-related inhibition of basal and pentagastrin-stimulated acid output (M.A.O.) with an estimated ID50 of 40 mg for the latter. In eight subjects with duodenal ulceration single 100 mg and 200 mg doses produced 85% and 97% inhibition of M.A.O. at peak (3 h post-dose) and 20% and 23% inhibition at 24 h, respectively; inhibition of basal acid output was 97% at 3 h and 50% at 24 h with both doses [1]. One hundred and thirty-five patients were randomly allocated to 4 weeks' treatment with either 150 mg zaltidine once daily or placebo. Fifty-nine were treated for a full 4 weeks with zaltidine before the trial was stopped. Healing rates after 4 weeks of zaltidine and placebo were 86% and 19%, respectively (p less than 0.001) [2].
Mapenterol-d6 hydrochloride is the deuterium labeled Mapenterol hydrochloride. Mapenterol hydrochloride is a type of β2-adrenoceptor agonist[1][2].