Piribedil dihydrochloride is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil dihydrochloride is also a α2-adrenoceptors antagonist. Piribedil dihydrochloride can inhibit MLL1 methyltransferase activity (EC50: 0.18 μM). Piribedil dihydrochloride has the potential for the research of parkinson's disease, circulatory disorders, cancers[1][2][3][4].
L-Epinephrine is a hormone secreted by the medulla of the adrenal glands. L-Epinephrine is an α-adrenergic and β-adrenergic receptor agonist.
Celiprolol hydrochloride is a potent, selective and orally active antagonist of β1-andrenoceptor with partial β2 agonist activity, therefore it is a selective adrenoreceptor modulator (SAM). Celiprolol hydrochloride demonstrates antihypertensive and antianginal activity[1].
Brimonidine (UK 14304) is a full α2-adrenergic receptor (α2-AR) agonist.
Ro 363 is a potent and highly selective β1-adrenoceptor agonist. RO 363 is an effective inotropic stimulant, and is a cardiovascular modulator that reduces diastolic blood pressure and pronounces increases in myocardial contractility[1][2][3].
RS 17053 hydrochloride is a potent and selective α1A adrenoceptor antagonist, with a pKi value of 9.1 in native cell membrane and a pA2 value of 9.8 in functional assays.
L-749372 is the beta 3 adrenergic receptor 3-Pyridyloxypropanolamine agonist.
Lofexidine hydrochloride is an α2A-adrenergic receptor agonist, commonly used to alleviate the physical symptoms of heroin and other types of opioid withdrawal.
Ritodrine hydrochloride (DU21220 hydrochloride) is a β-2 adrenergic receptor agonist.Target: β-2 Adrenergic ReceptorRitodrine is a tocolytic drug, used to stop premature labor. Ritodrine can significantly prolong a short interval more quickly but with relatively more side effects than magnesium sulphate. Stratified RCTs for different gestational ages and different labour stages should be designed for further study [1]. Ritodrine is a beta-2 adrenergic receptor agonist - a class of medication used for smooth muscle relaxation. Since ritodrine has a bulky N-substituent, it has high β2-selectivity. Also, the 4'-hydroxy on the benzene ring is important for activity as it is needed to form hydrogen bonds. However, the 4'-hydroxy makes it susceptible to metabolism by COMT. Since it is β2-selective it is used for premature labor [2].
Teoprolol is a β-adrenergic receptor blocker.
Hydrocortisone 17-butyrate is an adrenocortico hormone
Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5.
Perphenazine dihydrochloride is an orally active dopamine receptor and histamine-1 receptor antagonist, with Ki values of 0.56 nM (D2), 0.43 nM (D3), .6 nM (5-HT2A), respectively. Perphenazine dihydrochloride also binds to Alpha-1A adrenergic receptor. Perphenazine dihydrochloride inhibits cancer cell proliferation, and induces apoptosis. Perphenazine dihydrochloride can be used in the research of mental disease, cancer, inflammation[1][3][5].
Yohimbine is a potent and relatively nonselective alpha 2-adrenergicreceptor (AR) antagonist, with IC50 of 0.6 μM. IC50 value: 0.6 uM [1]Target: alpha 2-adrenergic receptorin vitro: Yohimbine inhibits alpha2-receptor antagonist with Ki of 1.05 nM, 1.19 nM, and 1.19 nM for α2A, α2B, α2C, respectively. Yohimbine also inhibits 5-HT1B with Ki of 19.9 nM. Yohimbine acts to block the lowering of cAMP by alpha-2 adrenoceptor agonists. yohimbine actually causes a pronounced lowering of tyrosinase activity. [3]in vivo: Yohimbine is an antagonist at alpha2-noradrenaline receptors with putative panicogenic effects in human subjects, was administered to Swiss-Webster mice at doses of 0.5, 1.0, and 2.0 mg/kg. Yohimbine potentiates active defensive responses to threatening stimuli in Swiss-Webster mice.[2]
Dabuzalgron (Ro 115-1240) is an orally active and selective α-1A adrenergic receptor agonist for the treatment of urinary incontinence. Dabuzalgron protects against Doxorubicin-induced cardiotoxicity by preserving mitochondrial function[1].
BMY 14802 is a sigma-1 receptor (σ1R) antagonist, as well as an agonist at serotonin (5-HT) 1A and adrenergic alpha-1 receptors. BMY 14802 inhibits abnormal involuntary movement (AIM) in rat Parkinson's disease (PD) model, with down-regulating the expression of AIM[1][2].
L-765314 is a potent and selective α1b adrenergic receptor antagonist with Kis of 5.4 nM and 2.0 nM for rat and human α1b adrenergic receptor, respectively.
Sibenadet hydrochloride (AR-C68397AA) is a dual D2 dopamine receptor, beta2-adrenoceptor agonist with bronchodilator activity. Investigation in animal models of key chronic obstructive pulmonary disease (COPD) symptoms has demonstrated that Sibenadet hydrochloride effectively inhibits sensory nerve activity, thereby reducing reflex cough, mucus production and tachypnoea.
Midaglizole ((±)-DG5128 free base, DG5128 free base) is a potent α2-adrenoceptor antagonist. Midaglizole is a hypoglycemic agent. Midaglizole increases blood pressure and reduces blood glucose levels in vivo[1][2][3].
(R)-Carvedilol-d4 is deuterium labeled (R)-Carvedilol. (R)-Carvedilol ((R)-BM 14190), the R-enantiomer of Carvedilol, is a non-selective β/α-1 blocker. (R)-Carvedilol exerts protection against the vascular or cardiac toxicity of Doxorubicin (DOX)[1].
Clozapine (HF 1854) is an antipsychotic used to treat schizophrenia. Clozapine is a potent antagonist of dopamine and a number of other receptors, with a Ki of 9.5 nM for M1 receptor.
Adrenaline sulfate is a orally active hormone secreted by the medulla of the adrenal glands. Adrenaline sulfate is an α-adrenergic and β-adrenergic receptor agonist. Adrenaline sulfate can be used in the treatment of anaphylaxis. Adrenaline sulfate has the potential for the research of cardiac arrest[1][2][3][4].
Landiolol hydrochloride (ONO1101 hydrochloride) is a highly beta1 selective ultra-short acting beta-blocker (β1/β2 selectivity = 255:1, a half-life of 4 min)， acts as an adrenoceptor antagonist[1].
Formoterol-d3 is deuterium labeled Arformoterol. Arformoterol ((R,R)-Formoterol), the (R,R)-enantiomer of Formoterol, is a long-acting β2-adrenergic receptor (β2-AR) agonist, with a Kd of 2.9 nM. Arformoterol can be used for the research of chronic obstructive pulmonary disease (COPD)[1][2].
(4E)-SUN9221 is a potent antagonist of α1-adrenergic receptor and 5-HT2 receptor, with antihypertensive and anti-platelet aggregation activities.
Abediterol (LAS100977) is an inhaled long-acting β2-adrenoceptor agonist (LABA) and can be used for the research of asthma and chronic obstructive pulmonary disease (COPD)[1].
Vilanterol is a long-acting β2-adrenoceptor (β2-AR) agonist with 24 h activity. The pEC50s for β2-AR,β1-AR and β3-AR is 10.37±0.05, 6.98±0.03 and 7.36±0.03, respectively.
Naftopidil (Flivas), a selective α1-adrenergic receptor antagonist or alpha blocker, is an antihypertensive drug.Target: α1-Adrenergic ReceptorNaftopidil significantly improved the overall international prostatic symptom score ; from 19.2±7.9 to 11.7±5.8 in the M group and from 19.4±6.4 to 12.3±6.8 in the E group (p<0.0001), QOL score from 4.9±0.8 to 3.2±1.4 in the M group and from 5.0±0.8 to 3.6±1.3 in the E group (p<0.0001), and OAB symptom score from 7.8±2.6 to 5.0±2.5 in the M group (p<0.0001) and from 8.6±2.9 to 5.8± 3.3 in the E group (p<0.0001). naftopidil improves storage symptoms as well as voiding symptoms regardless of timing of administration [1]. The selectivity of naftopidil for prostatic pressure was the most potent among the test compounds. In addition, using cloned human alpha1-adrenoceptor subtypes, naftopidil was selective for the alpha1d-adrenoceptor with approximately 3- and 17-fold higher affinity than for the alpha1a- and alpha1b-adrenoceptor subtypes, respectively. The selectivity of naftopidil for prostatic pressure may be attributable to its high binding affinity for alpha1a- and alpha1d-adrenoceptor subtypes [2].
Dipivefrin is a potent adrenergic agonist. Dipivefrin is an adrenergic pro-drug. Dipivefrin can be used for reduce IOP (intraocular pressure) in patients suffering from chronic open angle glaucoma[1][2].
Silodosin-d4 (KAD 3213-d4) is the deuterium labeled Silodosin. Silodosin (KAD 3213) is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker. Silodosin exhibits high affinity for α1A-AR (Ki=0.036 nM), over 162-fold and 50-fold than for α1B-AR and α1D-AR with Ki values of 21 nM and 2.0 nM, respectively. Silodosin is an effective and well-tolerated agent, it can be used for the investigation of LUTS/BPH[1][3].