Scopine is the metabolite of anisodine, which is a α1-adrenergic receptor agonist and used in the treatment of acute circulatory shock. Target: α1-Adrenergic ReceptorScopine is a tropane alkaloid found in a variety of plants including Mandragora root, Senecio mikanoides (Delairea odorata), Scopolia carniolica and Scopolia lurida. Scopine can be prepared by the hydrolysis of scopolamine. From Wikipedia.
Acetylneurotensin-(8-31) is the shortest analog of neurotensin with full binding and pharmacological activities[1].
Imiloxan hydrochloride is a potent and selective alpha 2B-adrenoceptor antagonist. Imiloxan hydrochloride has the potential for acute kidney injury research[1][2].
L-DOPA (Levodopa) sodium is an orally active metabolic precursor of neurotransmitters dopamine. L-DOPA sodium can cross the blood-brain barrier and is converted into dopamine in the brain. L-DOPA sodium has anti-allodynic effects, and can be used for Parkinson's disease research[1][2][3].
Sulamserod is a 5-HT4 receptor antagonist, with antiarrhythmic activities.
Levobunolol (l-Bunolol) is a potent and nonselective β-adrenergic receptor antagonist. Levobunolol is an ocular hypotensive agent and lowers mean intraocular pressure (IOP). Levobunolol can be used for glaucoma and superior oblique myokymia (SOM) research[1][2][3].
Chlorpheniramine-d4 (maleate) is deuterium labeled Chlorpheniramine (maleate).
Naltrindole hydrochloride is a highly potent and selective non-peptide δ opioid receptor antagonist with a Ki of 0.02 nM.
CP-135807 is an orally active and selective 5-HT1D agonist (IC50=3.1 nM), bovine). CP-135807 mediates central psychoactivity and can be used in antidepressant research[1][2].
TC-O 9311 is a potent orphan G protein-coupled receptor 139 (GPR139) agonist with an EC50 of 39 nM[1].
GSK 1562590 hydrochloride is a high affinity and selective antagonist of urotensin-II receptor (UT), with pKis of 9.14-9.66 for mammalian recombinant (mouse, rat, cat, monkey, human) and native UT[1].
Mebhydrolin is a specific histamine H1 receptor antagonist.
Tau-aggregation-IN-1 (Compound D-519) is a tau441 protein aggregation inhibitor with an IC50 of 21 µM. Tau-aggregation-IN-1 is also a dopamine D2 and D3 receptor agonist[1].
(Rac)-Nebivolol-d4 ((Rac)-R 065824-d4) is a labelled racemic Nebivolol. Nebivolol selectively inhibits β1- adrenergic receptor with IC50 of 0.8 nM[1][2].
Vofopitant dihydrochloride (GR 205171A) is a potent, selective and orally available tachykinin neurokinin 1(NK1) receptor antagonist, inhibits [3H]SP binding to the NK1 receptor with pKi values of 9.5 and 10.6 in rat and human membranes respectively, acts as a potential broad-spectrum anti-emetic agent[1].
CXCR4 modulator-2 (compound Z7R) is a highly potent CXCR4 modulator with an IC50 value of 1.25 nM. CXCR4 modulator-2 has acceptable stability (t1/2 = 77.1 min) in mouse serum and exhibits anti-inflammatory activity in mouse edema model[1].
mAChR-IN-1 hydrochloride is a potent muscarinic cholinergic receptor (mAChR) antagonist, with an IC50 of 17 nM[1].
Pramipexole (N-Propyl-3,3,3-d3) dihydrochloride is the deuterium labeled Pramipexole. Pramipexole is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS)[1][2][3].
GSK345931A is an EP1 receptor antagonist. GSK345931A shows measurable CNS penetration in the mouse and rat and potent analgesic efficacy in acute and sub-chronic models of inflammatory pain[1].
Kuwanon G is a flavonoid isolated from Morus alba, acts as a bombesin receptor antagonist, with potential antimicrobial activity[1][2].
Apomorphine is an orally active agonist of Dopamine receptor. Apomorphine can be used in study Parkinson, biphasic dyskinesias, urinary dysfunction,,dystonia, dyspnoea, anismus and belching[1].
Esmolol-d7 hydrochloride is the deuterium labeled Esmolol hydrochloride. Esmolol hydrochloride is a beta adrenergic receptor blocker[1][2].
VU0652835 is a metabotropic glutamate receptor subtype 5 (mGlu5) negative allosteric modulator with an IC50 of 81 nM[1].
RTICBM-189 is a potent, brain-penetrant allosteric modulator of the cannabinoid type-1 (CB1) receptor with a pIC50 of 7.54 in Ca2+ mobilization assay. RTICBM-189 has pIC50s of 5.29 and 6.25 for hCB1 and mCB1, respectively. RTICBM-189 significantly and selectively attenuates the reinstatement of the cocaine-seeking behavior in rats[1].
Dobutamine Hcl(Dobutrex) is a sympathomimetic drug used in the treatment of heart failure and cardiogenic shock. Its primary mechanism is direct stimulation of β1 receptors of the sympathetic nervous system.
Repinotan hydrochloride (BAY x 3702) is a potent, selective, brain-penetrant and orally active 5-HT1A receptor agonist, with Ki values of 0.19 nM (calf hippocampus), 0.25 nM (rat and human cortex), and 0.59 nM (rat hippocampus Repinotan hydrochloride has a weak affinity for other related receptors. Repinotan hydrochloride has pronounced neuroprotective effects[1].
Camylofin is an antimuscarinic, is a smooth muscle relaxant
Phentolamine is a potent, selective and orally active α1 adrenergic and α2 adrenergic receptor antagonist. Phentolamine can be used for the treatment of erectile dysfunction[1][2][3].
[D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P, a Substance P derivative, is a biased agonist toward neuropeptide and chemokine receptors. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P activates G12. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P binds to IL-8 and GRP receptors. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P inhibits ERK-2 activation, activates JNK activity. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P stimulates an increase in neutrophil migration and Ca2+ mobilization. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P is also a bombesin antagonist, and inhibits the growth of small cell lung cancer[1][2][3]
DCG-IV is a potent agonist of group II mGluRs with EC50s of 0.35 and 0.09 μM for mGlu2R and mGlu3R, reapectively. DCG-IV is also a competitive antagonist at group I (IC50: mGlu1R/5R=389/630 μM) and III receptors (IC50: mGlu4R/6R/7R/8R= 22.5/39.6/40.1/32 μM). DCG-IV has anticonvulsive and neuroprotective effects[1][2].