Renzapride (BRL 24924), a substituted benzamide, is a full 5-HT4 receptor agonist with a Ki value of 115 nM. Renzapride (BRL 24924) is also a 5HT2b and 5HT3 receptor antagonist[1]. Renzapride could be used for constipation predominant irritable bowel syndrome (C-IBS) study[2].
Etilefrine (3-[2-(ethylamino)-1-hydroxyethyl]phenol) is an α adrenergic agonist[2]. Etilefrine also is an AMPK activator[1]. Etilefrine can be used for the research of postural hypotension[3].
Kobe0065 is a novel and effective inhibitor of Ras-Raf interaction, competitively inhibiting the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46±13 μM.
A highly potent, subtype-selective melanin concentrating hormone receptor 1 (MCHR1) inhibitor with Ki of 17 nM, without inhibitory activity for MCHR2 at 10 uM; exhibits functional potency with Kb of 117 nM in FLIPR-based assay, with no activity for MCHR2 at 10 uM, dose-dependently reduces body weight in a chronic diet-induced obese model.
Idalopirdine (Lu AE58054) is a potent and selective 5-HT6 receptor antagonist with a Ki of 0.83 nM.
Sabcomeline (hydrochloride) is a potent and functionally selective muscarinic M1 receptor partial agonist that improve cognition.
Valsartan-d3 is the deuterium labeled Valsartan[1]. Valsartan (CGP 48933) is an angiotensin II receptor antagonist and has the potential for high blood pressure and heart failure research[2].
Atropine (Tropine tropate) hydrobromide is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine hydrobromide inhibits ACh-induced relaxations in human pulmonary veins. Atropine hydrobromide can be used for research of anti-myopia and bradycardia[1][2][3][4].
Meclinertant (SR 48692) is a potent, selective, nonpeptide and orally active neurotensin receptor 1 (NTS1) antagonist. In human colon carcinoma (HT-29) cells, Meclinertant competitively antagonizes neurotensin-induced intracellular Ca2+ mobilization with a pA2 values of 8.13. Meclinertant has anxiolytic, anti-addictive and memory-impairing effects[1][2][3].
Clozapine N-oxide (CNO) is a major metabolite of the anti-psychotic drug clozapine. Clozapine N-oxide is a agonist for the chemogenetic Designer Receptors Exclusively Activated by Designer Drug (DREADD) system.
CALP1 is a calmodulin (CaM) agonist (Kd of 88 µM) with binding to the CaM EF-hand/Ca2+-binding site. CALP1 blocks calcium influx and apoptosis (IC50 of 44.78 µM) through inhibition of calcium channel opening. CALP1 blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 activates CaM-dependent phosphodiesterase activity[1][2][3][4].
Antide (D-21074) is a potent LHRH antagonist. Antide also can be used for the research of prostatic cancer.
Frovatriptan succinate ((R)-Frovatriptan succinate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate has the potential for migraine research[1][2].
Tetrahydropalmatine, an active component isolated from corydalis, acts through inhibition of amygdaloid release of dopamine to inhibit an epileptic attack in rats.
Setiptiline-d3 (Org-8282-d3) is the deuterium labeled Setiptiline. Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine[1][2].
MMPIP hydrochloride is an allosteric metabotropic glutamate receptor 7 (mGluR7) selective antagonist (KB values 24 -30 nM). MMPIP hydrochloride acts as a pharmacological tool for elucidating the roles of mGluR7 on central nervous system functions. MMPIP hydrochloride alleviates pain and normalizes affective and cognitive behavior in neuropathic mice[1][2].
Lys-Bradykinin, a kind of kallidin and bradykinin receptor ligand, can be generated by kininogen protein through enzymatic cleavage by the protease kallikrein. Lys-Bradykinin, also a vasodilator, can widen blood vessels and increase blood flow. Lys-Bradykinin involves in vascular regulation, inflammation and pain sensation[1].
Trebananib (2xCon4C; AMG 386), a non-VEGF-dependent angiogenesis pathway inhibitor, is a peptide-Fc fusion protein that neutralises the interaction between angiopoietins-1/2 and the Tie2 receptor, plus FOLFIRI. Trebananib can be used to research anticancer and ocular neovascular diseases[1][2].
Levosulpiride (RV-12309) is the (S)-enantiomer of sulpiride, which is a D2 receptor a antagonist, an atypical antipsychotic drug of the benzamide class.
Ciproxifan maleate(FUB-359 maleate) is a highly potent and selective histamin H3-receptor antagonist with IC50 of 9.2 nM, with low apparent affinity at other receptor subtypes.IC50 value: Target: H3 receptorIn vitro, Ciproxifan behaved as a competitive antagonist at the H3 autoreceptor controlling 3H histamine release from synaptosomes and displayed similar Ki values (0.5-1.9 nM) at the H3 receptor controlling the electrically-induced contraction of guinea pig ileum or at the brain H3 receptor labeled with 125I-iodoproxyfan. This appears to be an orally bioavailable, extremely selective and potent H3-receptor antagonist whose vigilance- and attention-promoting effects are promising for therapeutic applications in aging disorders.
Bisoprolol is a selective type β1 adrenergic receptor blocker.Target: Adrenergic ReceptorApproved: July 31, 1992Bisoprolol, on beta 1-adrenoceptor peptide induced autoimmune myocardial damage. In the animal model of autoimmune cardiomyopathy induced by active immunization of rabbits with beta 1-adrenoceptor peptide, bisoprolol was given at a dose of 3 mg/day throughout the study period. Our results showed high titer of anti-beta 1-adrenoceptor antibody in the immunized group throughout the study but not in the group receiving only bisoprolol [1]. Bisoprolol administration resulted in a significant reduction in HR reaching 60.3 +/- 1.4 bpm at VT of 500 mL (compared to 70.5 +/- 1.8 bpm with placebo, P < 0.001). Changes in HP were also significant with an increase in HP reaching 1004.5 +/- 22.2 msec at this controlled VT (compared to 860.3 +/- 21.5 msec with placebo, P < 0.001) [2].Toxicity: Oral, mouse: LD50 = 100 mg/kg; Skin, rabbit: LD50 = 200 mg/kg; Skin, rat: LD50 = 500 mg/kg. Symptoms of overdose include congestive heart failure (marked by sudden weight gain, swelling of the legs, feet, and ankles, fatigue, and shortness of breath), difficult or labored breathing, low blood pressure, low blood sugar, and slow heartbeat.
FR 113680 is a tripeptide substance P antagonist that interacts selectively with the NK1 neurokinin receptor[1].
pan-KRAS-IN-2 (compound 6) is a pan inhibitor of with IC50s ≤10 nM for KRAS WT and mutants (G12D, G12C, G12V, G12S, G12A, Q61H), and ＞10 μM for KRAS G13D, respectively[1].
Besipirdine is a non-receptor-dependent cholinomimetic agent with noradrenergic activity. Besipirdine inhibits voltage-dependent sodium and potassium channels.
L-741626 is a selective D2 dopamine receptor antagonist, with the Ki values of 2.4, 100 and 220 nM for human D2, D3 and D4 receptors respectively[1].
W-84 (dibromide) is a potent allosteric modulator of M2-cholinoceptors, which retards [3H]N-methylscopolamine dissociation. W-84 dibromide can stabilize cholinergic antagonist-receptor complexes. W-84 (dibromide) is a non-competitive muscarinic acetylcholine receptors antagonist with allosteric effects. W-84 (dibromide) protects over additively against an organophosphate-intoxication when applied in combination with atropine[1][2][3].
Lu AA33810 is a potent and selective antagonist of neuropeptide Y5 receptor with a Ki of 1.5 nM for the human receptor. Lu AA33810 exhibts antianxiolytic-like and antidepressant-like effects[1].
Methyldopa is an alpha-adrenergic agonist (selective for α2-adrenergic receptors) psychoactive drug used as a sympatholytic or antihypertensive.Target: alpha-adrenergic agonistMethyldopa is an alpha-adrenergic agonist (selective for α2-adrenergic receptors) psychoactive drug used as a sympatholytic or antihypertensive. Its use is now mostly deprecated following the introduction of alternative safer classes of agents. However, it continues to have a role in otherwise difficult to treat hypertension and gestational hypertension (also known as pregnancy-induced hypertension (PIH)).Methyldopa has a dual mechanism of action. It is a competitive inhibitor of the enzyme DOPA decarboxylase, also known as aromatic L-amino acid decarboxylase, which converts L-DOPA into dopamine. Dopamine is a precursor for norepinephrine (noradrenaline) and subsequently epinephrine (adrenaline). This inhibition results in reduced dopaminergic and adrenergic neurotransmission in the peripheral nervous system. This effect may lower blood pressure and cause central nervous system effects such as depression, anxiety, apathy, anhedonia, and parkinsonism. It is converted to α-methylnorepinephrine by dopamine beta-hydroxylase (DBH). α-methylnorepinephrine is an agonist of presynaptic central nervous system α2-adrenergic receptors. Activation of these receptors in the brainstem appears to inhibit sympathetic nervous system output and lower blood pressure. This is also the mechanism of action of clonidine.
Prifinium bromide is antimuscarinic agent with antispasmodic, antiemetic effect[1].
N6-Cyclopentyladenosine (CPA) is a selective Adenosine A1 receptor agonist, with Ki values of 2.3 nM, 790 nM and 43 nM for human A1, A2A and A3 receptors, respectively[1][2].