A novel potent soluble guanylate cyclase (sGC) activator; reduces progression of renal damage in the ZSF1 rat, shows the potential as an effective therapy for diabetic nephropathy.
Ecastolol is a beta adrenergic receptor antagonist, with antianginal activities.
AMG-510 racemate is the racemate of AMG-510. AMG-510 is a potent KRAS G12C covalent inhibitor.
Sofpironium bromide (BBI 4000) is an anticholinergic agent used in the study of primary axillary hyperhidrosis (PAH). Sofpironium bromide reduces sweating by inhibiting M3 muscarinic receptors in eccrine glands at the application site. Sofpironium bromide also has a high afnity for the M1, M2, M4 and M5 subtypes[1].
DuP 734 is a sigma receptor antagonist. DuP 734 is a selective and potent sigma and 5-HT2 receptor ligand with weak affinity for D2 receptors. DuP 734 may have antipsychotic activity without the liability of motor side effects typical of neuroleptics[1][2][3].
PSB 0474 (3-phenacyl-UDP) is a selective and potent P2Y6 receptor agonist with an EC50 of 70 nM[1]. PSB 0474 inhibits cell proliferation, increases NO release in astrocytes and microglia cells. PSB 0474 induces astrocytes apoptosis[2].
Tropicamide is an anticholinergic and a muscarinic receptor subtype M4-preferring antagonist .Target: mAChRTropicamide is an antimuscarinic drug that produces short acting mydriasis (dilation of the pupil) and cycloplegia when applied as eye drops. It is used to allow better examination of the lens, vitreous humor, and retina. Due to its relatively short duration of effect (4-8 hours), it is typically used during eye examinations such as the dilated fundus examination, but it may also be used before or after eye surgery. Cycloplegic drops are often also used to treat anterior uveitis, decreasing risk of posterior synechiae and decreasing inflammation in the anterior chamber of the eye [1-3].
TFLLR-NH2 (TFA) is a selective PAR1 agonist with an EC50 of 1.9 μM.
Alverine citrate is a 5-HT1A receptor antagonist, with an IC50 of 101 nM.
Opigolix is a Gonadotropin-releasing hormone (GnRH) receptor antagonist, used for the research of endometriosis and rheumatoid arthritis.
(S)-Carvedilol, the S-enantiomer of Carvedilol, is a non-selective β/α-1 blocker. (S)-Carvedilol exerts protection against the vascular or cardiac toxicity of Doxorubicin (DOX)[1].
Dp[Tyr(methyl)2,Arg8]-Vasopressin is a non-selective peptide arginine vasopressin Vlb receptor antagonist[1].
VU-29 is a positive allosteric modulator of metabotropic glutamate 5 (mGlu5) receptor (EC50=9 nM and Ki=244 nM for rmGluR5). VU-29 is selective for mGluR5 relative to other mGluR subtypes (EC50: rmGluR1/rmGluR2=557 nM/1.5 μM; hmGluR4=154 nM)[1][2].
Deucrictibant is a potent bradykinin receptor antagonist. Bradykinin receptors are cell surface, G-protein coupled receptors of the seven-transmembrane domained family[1].
YM-46303 is an mAChR antagonist which exhibits the highest affinities for M1 and M3 receptors, and selectivity for M3 over M2 receptor.
Ebastine(LAS-W 090;RP64305) is a long-acting and selective H1-histamine receptor antagonist.Target: Histamine H1 ReceptorEbastine is a H1 antihistamine with low potential for causing drowsiness. Ebastine (10 mg orally) causes brain histamine H1-receptor occupation of approximately 10%, consistent with its lower incidence of sedative effect, whereas (+)-chlorpheniramine occupied about 50% of brain H1-receptors even at a low but sedative dose of 2 mg; occupancy of (+)-chlorpheniramine was correlated with plasma (+)-chlorpheniramine concentration [1]. ebastine 10 or 20 mg once daily was rapidly effective in relieving symptoms of PAR in adult and adolescent patients; additional benefits of the 20-mg dose became apparent in the longer term [2]. ebastine is an effective and generally well-tolerated treatment for allergic rhinitis and chronic idiopathic urticaria. In addition to the regular tablet formulation, ebastine is available as a FDT, providing a treatment option that is particularly convenient for patients [3].
Degarelix acetate hydrate is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR/LHRHR) antagonist. Degarelix acetate hydrate can be used for prostate cancer research[1].
Taranabant racemate is an antagonist and/or inverse agonist of the Cannabinoid-1 (CB1) receptor extracted from patent WO 2004048317 A1.
Azilsartan mepixetil is the antagonist of angiotensin II receptor. Azilsartan mepixetil has stronger and longer blood pressure effect, more abvious and longer lasting heart rate lowering effect and high safety. Azilsartan mepixetil achieves ideal protective effect for heart and kidney functions. Azilsartan mepixetil has the potential for the research of hypertension, chronic heart failure and diabetic nephropathy (extracted from patent CN107400122A)[1].
LY2828360 is a slowly acting but efficacious G protein-biased cannabinoid (CB2) agonist, inhibiting cAMP accumulation and activating ERK1/2 signaling.
M1 ligand 1 (compound 3b-b) is a muscarinic acetylcholine receptor M1 ligand. M1 ligand 1 is a N-desmethyl congener of arecoline derivative. M1 ligand 1 can be used as PET (positron emission tomography) radiotracer[1].
VU0361747 is a positive allosteric modulators (PAM) of metabotropic glutamate receptor subtype 5 (mGlu5).
Iodophenpropit dihydrobromide is a potent and selective histamine H3 receptor antagonist. The binding of [125I]Iodophenpropit is selective, saturable, readily reversible, and of high affinity (KD 0.32 nM)[1].
Rezatomidine (AGN-203818) is a potent and selective α2-AR agonist. Rezatomidine can be used for diabetic neuropathy and neuropathic pain research[1].
LY2624803 is a novel potent histamine H1 and 5HT-2A receptor modulator in the pipeline for treating insomnia. Sleep Disorder Phase 2 Discontinued
Etersalate inhibits platelet function and decreases thromboxane A2 (TXA2) levels.
Ranitidine is a histamine H2-receptor antagonist that inhibits stomach acid production. Target: Histamine H2-ReceptorRanitidine (Zantac) is a histamine H2-receptor antagonist with IC50 of 3.3 ± 1.4 uM. It inhibits stomach acid production. It is also used alongside fexofenadine and other antihistamines for the treatment of skin conditions such as hives. It has 10% the affinity that cimetidine has to CYP450 so it causes fewer side effects, but other H2 blockers famotidine and nizatidine have no CYP450 significant interactions [1, 2].
Ethamsylate is a haemostatic drug, also inhibits biosynthesis and action of those prostaglandins.
AH-7614 is a potent and selective FFA4 antagonist, with pIC50s of 7.1, 8.1, and 8.1 for human, mouse, and rat FFA4, respectively. AH-7614 has selectivity for FFA4 over FFA1 (pIC50<4.6). AH-7614 is also a negative allosteric modulator (NAM) of FFA4. AH-7614 is able to block effects of both the polyunsaturated ω-6 fatty acid linoleic acid and the synthetic FFA4 agonist[1][2].
Salbutamol Hemisulfate is a short-acting β2 adrenergic receptor agonistTarget: β2 Adrenergic ReceptorSalbutamol is a short-acting, selective beta2-adrenergic receptor agonist used in the treatment of asthma and COPD. All the effects of R,S-salbutamol on guinea-pig skeletal muscles are due to the activity of the R-enantiomer. Thus there is a common enantiomeric profile for the skeletal muscle and bronchorelaxant activity of the compound [1]. Short-term Salbutamol intake did appear to improve performance during intense submaximal exercise with concomitant increase in substrate availability and utilization, but the exact mechanisms involved need further investigation [2]. Short-term administration of salbutamol increases voluntary muscle strength in man. However, the magnitude and duration of this effect vary between muscle groups. This study implies that the beta 2-adrenoceptor agonists may be of therapeutic potential in altering skeletal muscle function in humans [3].