[Leu3]-Oxytocin, an oxytocin analogue, is derived by structural variation in sequence position 3 replaced by leucine (Leu)[1].
3,4-Dimethoxyphenol is a plant-derived phenylpropanoid compound and can use as a whitening agent in cosmetics. 3,4-Dimethoxyphenol has tyrosinase-inhibiting activity[1]. 3,4-Dimethoxyphenol has potent antioxidant effect isolated from the bacterial fermentation broth[2].
Gastric Inhibitory Peptide, porcine is a glucose-dependent insulinotropic polypeptide, is a 42 amino acid intestinal hormone with effects on fat and glucose metabolism[1].
[D-Phe2,6, Pro3]-LH-RH is a potent luteinizing hormone releasing hormone (LHRH) antagonist[1].
Altrenogest(A35957; RU2267) is a progestogen structurally related to veterinary steroid trenbolone.Target: Progesterone ReceptorAltrenogest is a progestogen structurally related to veterinary steroid trenbolone. Treatment of embryo-recipient mares with altrenogest appears to be beneficial in extending the degree of donor-recipient synchrony required for successful embryo transfer. Altrenogest treatment also seems to be conductive to pregnancy maintenance in recipients experiencing luteal dysfunction [1]. The oil and gel altrenogest preparations are equally effective in modulating estrous behavior and time to estrus and ovulation. Altrenogest treatment started late in diestrus appears to result in a high incidence of ovulation during treatment and when luteolysis and ovulation occur during treatment; the subsequent luteal phase is frequently prolonged due to failure of regression of the CL [2].
Clomifene Citrate is a selective estrogen receptor modulator.Target: Estrogen Receptor/ERRClomifene Citrate(CC) acted as an estrogen antagonist regardless of the concentration of E2 added together. In conclusion, CC acts as an estrogen agonist/antagonist via ER alpha in a coexisting estrogen concentration-dependent way whereas it acts as an estrogen antagonist via ER beta whether or not estrogen is present [1]. Clomiphene was effective in increasing pregnancy rate compared to placebo (OR 5.8, 95% CI 1.6 to 21.5) as was clomiphene plus dexamethasone treatment (OR 9.46, 95% CI 5.1 to 17.7) compared to clomiphene alone. A significant improvement in the pregnancy rate was reported for clomiphene plus combined oral contraceptives versus clomiphene alone. No evidence of a difference in effect on pregnancy rate was found with any of the other comparisons [2].
Pheromonotropin (Pseudaletia separata) (Pss-PT) is an armyworm (Pseudaletia separata) pheromone with the C-terminal pentapeptide FXPRL-amide. Pheromonotropin (Pseudaletia separata) belongs to the PK/PBAN family and stimulates sex pheromone biosynthesis in moths, mediating feeding (intestinal muscle contraction), development (embryonic diapause, pupal diapause, and pupation), and defense against natural enemy insects wait[1].
Somatostatin is a tetradecapeptide which can suppress the growth hormone (GH) secretion and control the pituitary hormone secretion in human CNS.
Diphemanil methylsulfate is a quaternary ammonium anticholinergic. It binds muscarinic acetycholine receptors and thereby decreases secretory excretion of stomach acids as well as saliva and sweat.IC50 value: Target: mAChRDiphemanil Methylsulfate exerts its action by primarily binding the muscarinic M3 receptor. M3 receptors are located in the smooth muscles of the blood vessels, as well as in the lungs. This means they cause vasodilation and bronchoconstriction. They are also in the smooth muscles of the gastrointestinal tract (GIT), which help in increasing intestinal motility and dilating sphincters. The M3 receptors are also located in many glands which help to stimulate secretion in salivary glands and other glands of the body.
2-Thiouracil is a thiolated uracil derivative that is a known antihyperthyroid agent. Target: Others2-Thiouracil is an established antithyroid drug and an extensively investigated agent for the early detection and targeting of metastatic melanotic melanoma. In addition, 2-Thiouracil is also a selective inhibitor of neuronal nitric oxide synthase antagonising tetrahydrobiopterin-dependent enzyme activation and dimerization. Thiouracil refers both to a specific molecule consisting of a sulfated uracil, and a family of molecules based upon that structure. Thiouracil inhibits thyroid activity by blocking the enzyme thyroid peroxidase [1-3].
Terazosin hydrochloride is a quinazoline derivative and a competitive and orally active α1-adrenoceptor antagonist. Terazosin hydrochloride works by relaxing blood vessels and the opening of the bladder. Terazosin hydrochloride has the potential for benign prostatic hyperplasia (BPH) and high blood pressure treatment[1][2][3].
PAPA NONOate is a NO donor with a NO release half-life of 77 min (22-25°C). PAPA NONOate may represent a potential treatment for impaired wound healing in diabetes by increasing the rate of collagen synthesis at the wound site[1][2][3].
Exo2 is a secretion inhibitor. Exo2 perturbs trafficking of Shiga toxin between endosomes and the trans-Golgi network. Exo2 blocks secretory cargo exit from the ER (endoplasmic reticulum) and disrupts the Golgi apparatus, but does not affect the morphology of the TGN (trans-Golgi network) Exo2 can stimulate calcium-dependent exocytosis in permeabilized adrenal chromaff in cells[1][2].
Dobutamine tartrate is a synthetic catecholamine that acts on α1-AR, β1-AR, β2-AR (α-1, β-1 andβ-2 adrenoceptors). Dobutamine tartrate is a selective β1-AR agonist, relatively weak activity at α1-AR and β2-AR. Dobutamine tartrate can increase cardiac output and correct hypoperfusion[1][2][3][4].
Bremelanotide Acetate is a melanocortin agonist.IC50 value:Target: melanocortinin vivo: Bremelanotide is a novel drug candidate for the treatment of male and female sexual dysfunction. Bremelanotide has shown promise in effectively treating erectile dysfunction (ED) without the cardiovascular effects found in ED drugs currently available. Bremelanotide works through a mechanism of action involving the central nervous system rather than directly on the vascular system. As a result, it may offer significant safety and efficacy benefits over currently available products.
Alrestatin sodium is an inhibitor of aldose reductase, an enzyme involved in the pathogenesis of complications of diabetes mellitus, including diabetic neuropathy.
Idazoxan hydrochloride (RX 781094 hydrochloride) is an α2-adrenoceptor antagonist and is also a imidazoline receptors (IRs) antagonist competitively antagonized the centrally induced hypotensive effect of imidazoline-like drugs (IMs). Idazoxan hydrochloride also improves motor symptoms in Parkinson’s disease, L-DOPA-induced dyskinesias, and experimental Parkinsonism[1][2].
CHF-6366 is a potent M3 muscarinic antagonist and β2-adrenergic receptors agonist with pKi values of 10.4 and 11.4, respectively. CHF-6366 is also a weak calcium channel inhibitor (IC50~50 μM). CHF-6366 inhibits bronchoconstriction in guinea pigs. CHF-6366 can be used to research chronic obstructive pulmonary disease (COPD)[1].
Tripelennamine citrate, an ethylenediamine derivative, is a potent histamine H1-receptor antagonist. Tripelennamine citrate lessens the allergic response of the organism caused by histamine. Tripelennamine citrate can be used for the research of rhinitis, conjunctivitis, and allergic and anaphylactic reactions[1][2][3].
Metoprolol fumarate (CGP 2175C) is an orally active, selective β1-adrenoceptor antagonist. Metoprolol fumarate shows anti-inflammation, antitumor and anti-angiogenic properties[1][2][3].
Azoramide is a small-molecule modulator of the unfolded protein response with antidiabetic activity.in vitro: Azoramide is a dual-function endoplasmic reticulum (ER) modulator. Azoramide improves ER protein-folding ability and activates ER chaperone capacity to protect cells against ER stress in multiple systems. Azoramide regulates ER folding and secretion capacity without inducing ER stress. Azoramide might have the protective effects of enhancing chaperone expression and reducing protein synthesis without inducing cytotoxicity and apoptosis.in vivo: Azoramide exhibits potent antidiabetic efficacy in two independent mouse models of obesity by improving insulin sensitivity and pancreatic β cell function. Azoramide improves glucose homeostasis in mice with genetic obesity. Azoramide improves glucose homeostasis in mice with diet-induced obesity.
1,4-Diaminobutane-d8 (dihydrochloride) is the deuterium labeled 1,4-Diaminobutane dihydrochloride[1]. 1,4-Diaminobutane (Putrescine) dihydrochloride is an endogenous metabolite, acts as an indicator of pollution-induced stress in higher plants: barley and rape stressed with Cr(III) or Cr(VI)[2][3].
Iloprost-d4 (Ciloprost-d4) is the deuterium labeled Iloprost. Iloprost (ZK 36374) is a synthetic analogue of prostacyclin PGI2[1][2].
[D-Asn5]-Oxytocin possesses very low specific oxytocic and vasodepressor activities. By cumulative dose-response studies for oxytocic activity, [D-Asn5]-Oxytocin has similar intrinsic activity to oxytocin[1].
Promestriene is a synthetic diethyl-ether of estradiol and a locally effective estrogen. Promestriene has an efficient action on vaginal atrophy while it is minimally absorbed[1][2].
2-Hydroxyestrone (Catecholestrone) is a specific receptor-mediated antiestrogenic agent. 2-Hydroxyestrone is anticarcinogenic[1][2].
β-Estradiol 17-acetate is a metabolite of estradiol. Target: Othersβ-Estradiol 17-acetate is a metabolite of estradiol.
3,3',5-Triiodo-L-thyronine sodium is an active form of thyroid hormone, which binds to β1 thyroid hormone receptor (TRβ1), and activates its activity.
Phosphoglycerate kinase (PGK), namely phosphoglycerate kinase, is a glycolytic enzyme commonly used in biochemical research. Phosphoglycerate kinase can catalyze the reversible transfer of phosphate groups from 1,3-bisphosphoglycerate (1,3-BPG) to ADP to generate 3-phosphoglycerate (3-PG) and ATP. At the same time, it can also participate in gluconeogenesis, catalyzing the opposite reaction to produce 1,3BPGA and ADP. Phosphoglycerate kinase is involved in energy metabolism, interaction with nucleic acid, tumor progression, cell death and virus replication and other related processes[1].
rel-Tranylcypromine (SKF 385) is a potent monoamine oxidase (MAO) inhibitor[1].