D2343 is a β2-adrenoceptor agonist and also is an α1- adrenoceptor inhibitor.
Apraclonidine hydrochloride (ALO 2145), a selective α2 and weak α1 receptor agonist activity, effectively lowers intraocular pressure (IOP) in human eyes. Apraclonidine hydrochloride is a topical ophthalmic solution[1][2].
Pardoprunox(SLV-308) is a novel partial dopamine D2 and D3 receptor agonist and serotonin 5-HT1A receptor agonist; D2 (pKi = 8.1) and D3 receptor (pKi = 8.6) partial agonist (IA = 50% and 67%, respectively) and 5-HT1A receptor (pKi = 8.5) full agonist (IA = 100%); also binds to D4 (pKi = 7.8), α1-adrenergic (pKi = 7.8), α2-adrenergic (pKi = 7.4), and 5-HT7 receptors (pKi = 7.2) with lower affinity.IC50 value:Target:in vitro: SLV308 acted as a potent but partial D(2) receptor agonist (pEC(50) = 8.0 and pA(2) = 8.4) with an efficacy of 50% on forskolin stimulated cAMP accumulation. At human recombinant dopamine D(3) receptors, SLV308 acted as a partial agonist in the induction of [(35)S]GTPgammaS binding (intrinsic activity of 67%; pEC(50) = 9.2) and antagonized the dopamine induction of [(35)S]GTPgammaS binding (pA(2) = 9.0). SLV308 acted as a full 5-HT(1) (A) receptor agonist on forskolin induced cAMP accumulation at cloned human 5-HT(1) (A) receptors but with low potency (pEC(50) = 6.3) [1].in vivo: Unified PD Rating Scale (UPDRS)-Motor score was improved in pardoprunox-treated patients (overall mean dose 23.8 mg/d; -7.3 points), as compared with placebo (-3.0 points; P = 0.0001), from baseline to end point. At end point, there were more responders (> or = 30% reduction in UPDRS-Motor score) in the pardoprunox group (50.7%) than in the placebo group (15.7%; P < 0.0001) [2]. Surprisingly in the SNc, pardoprunox (10 μg kg?1, i.v.) either partially or fully suppressed the firing activity in two separate populations of DA neurons. Finally, in the DRN, pardoprunox (5-40 μg kg-1, i.v.) completely suppressed the firing activity of 5-HT neurons. Moreover, the selective 5-HT(1A) receptor antagonist WAY-100,635 prevented and reversed the effects of pardoprunox [3].
Butaxamine (Butoxamin) hydrochloride is a specific β2-adrenergic receptor blocker. Butaxamine hydrochloride inhibits the decreases in urine volume in ethanol-anesthetized, water-diuretic rats[1].
(Rac)-Dobutamine-d4 hydrochloride is a labelled racemic Dobutamine hydrochloride. Dobutamine hydrochloride is a synthetic catecholamine that acts on α1-AR, β1-AR, β2-AR (α-1, β-1 andβ-2 adrenoceptors). Dobutamine hydrochloride is a selective β1-AR agonist, relatively weak activity at α1-AR and β2-AR. Dobutamine hydrochloride can increase cardiac output and correct hypoperfusion[1][2][3][4].
N-Methyltyramine is a protoalkaloid that can be isolated from various plant species. N-Methyltyramine is an α2-adrenoreceptor antagonist. N-Methyltyramine enhances appetite and digestion of foods by stimulating gastrin and pancreatic secretions. N-Methyltyramine can relax mouse small intestinal smooth muscle and inhibits small intestinal propulsion[1][2].
Levobetaxolol hydrochloride is a beta-adrenergic receptor inhibitor (beta blocker), used to lower the pressure in the eye in treating conditions such as glaucoma.
Mibenratide, a small cyclic peptide, is an adrenergic β1 receptor antagonist. Mibenratide can be used for heart failure research[1].
Rezatomidine (AGN-203818) is a potent and selective α2-AR agonist. Rezatomidine can be used for diabetic neuropathy and neuropathic pain research[1].
Diacetolol D7 is a deuterium labeled Diacetolol. Diacetolol is the major metabolite of Acebutolol. Diacetolol is a β-adrenoceptor blocking and anti-arrhythmic agent[1].
B-HT 920(Talipexole 2Hcl) is a dopamine D2 receptor agonist, α2-adrenoceptor agonist and 5-HT3 receptor antagonist, which displays antiParkinsonian activity.IC50 Value: 25 nM(Adrenergic receptor α-2, rat)Target: Adrenergic Receptor; 5-HT Receptor; Dopamine Receptorin vitro: N/Ain vivo: Intravenous injection of 30 micrograms/kg of B-HT 920 into cats lead initially to an increase in blood pressure and then to a long-lasting decrease in blood pressure and heart rate. Vagally mediated reflex bradycardia elicited by angiotensin injection in beta-adrenoceptor-blocked dogs was facilitated by intracisternal injection of 10 micrograms/kg B-HT 920.
Xamoterol hemifumarate is a selective and potent agonist of beta1-adrenergic receptor. Xamoterol hemifumarate has the potential for the research of arrhythmogenesis. Xamoterol hemifumarate has the potential for the investigating the relationship between β1-adrenergic stimulation and IKr[1].
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].
Clenproperol is a β2-adrenergic agonist[1].
Zolertine hydrochloride is an α-adrenoceptor antagonist with a pKi of 6.81 in rat liver (α1B-adrenoceptors) and 6.35 in rabbit liver (α1A-adrenoceptors) membranes[1].
Naftopidil-d5 is deuterium labeled Naftopidil. Naftopidil (KT-611) is is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil has antiproliferative effects. Naftopidil can be used for the research of prostate hyperplasia[1][2].
Piribedil D8 is the deuterium labeled Piribedil, which is an antiparkinsonian agent.
Norfenefrine hydrochloride is an orally active, endogenously found α-adrenergic agonist and can be used for the research of female stress incontinence[1][2].
BODIPY FL prazosin is a fluorescent α1-adrenergic antagonist with Ki values of 14.5, 43.3 nM for α1a-AR and α1b-AR, respectively. BODIPY FL prazosin also is a fluorescent ligand with the excitation and emission wavelengths are 485 and 535 nm, respectively. BODIPY FL prazosin can be used for study the differences in the subcellular localization of α1-adrenoceptor subtypes[1][2][3].
Alfuzosin hydrochloride is an α1 adrenergic receptor antagonist used to treat benign prostatic hyperplasia (BPH).Target: α1 adrenergic receptorAlfuzosin, a new quinazoline derivative, acts as a selective and competitive antagonist of alpha 1-adrenoceptor-mediated contraction of prostatic, prostatic capsule, bladder base and proximal urethral smooth muscle, thereby reducing the tone of these structures. Consequently, urethral pressure and resistance, bladder outlet resistance, bladder instability and symptoms associated with benign prostatic hyperplasia are reduced. A limited range of clinical studies have shown oral alfuzosin to be more effective than placebo (in studies of < or = 6 months duration), to have sustained effects on long term administration (< or = 30 months), and to be comparable with the alpha 1-adrenoceptor antagonist prazosin, in the symptomatic treatment of benign prostatic hyperplasia.Oral alfuzosin 7.5 to 10 mg/day in divided doses appears to be a promising first-line agent for symptomatic treatment of noncomplicated mild to moderate benign prostatic hyperplasia in patients with a high dynamic component to their obstruction. In addition, alfuzosin offers an alternative to prostatectomy (the current 'gold standard') in patients who require surgery but are unfit for this treatment, and in patients requiring symptomatic relief while awaiting surgery.
Todralazine hydrochloride (Ecarazine hydrochloride) is an anti-hypertensive agent, acts as a β2AR blocker, with antioxidant and free radical scavenging activity[1].
JP1302 is a potent, selective, high affinity antagonist of the α2C-adrenoceptor, with a Kb of 16 nM and a Ki of 28 nM for the human α2C-receptor. JP1302 shows antidepressant and antipsychotic-like effects. JP1302 can be used for neuropsychiatric disorders and renal dysfunction research[1][2][3].
Oxyfedrine, a vasodilator, is an orally active β-adrenoreceptor agonist. Oxyfedrine decreases the tonicity of coronary vessels. Oxyfedrine can be used in the research of cardiovascular disease[1][2].
β3-AR agonist 1 (compound 15) is a highly potent, selective, and orally available β3-adrenergic receptor (β3-AR) agonist (EC50=18 nM), being inactive to β1-, β2-, and α1A-AR (β1/β3, β2/β3, and α1A/β3>556-fold)[1].
Phenylephrine-d6 (hydrochloride) is deuterium labeled Phenylephrine (hydrochloride). (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
Carazolol is a β1/β2 adrenoceptor antagonist of high potency used in the research of hypertension. Carazolol is also a potent, selective β3-adrenoceptor agonist[1].
Bromchlorbuterol hydrochloride is an active β-adrenergic agonist (β-agonist) and can be used for the research of pulmonary disease and asthma[1].
Naminterol is a phenethanolamine derivative, is a β2 adrenoceptor agonist with bronchodilatory properties. Naminterol is used for treatment of asthma.
Guanabenz (hydrochloride) is an oral α-2-adrenoceptor agonist, has antihypertensive effect and antiparasitic activity. Guanabenz (hydrochloride) interferes ER stress-signalling and has protective effects in cardiac myocytes. Guanabenz (hydrochloride) also is used for the research of high blood pressure(equivalent).
β2AR/M-receptor agonist-1 (example 131) is a muscarinic antagonist and β2 adrenoceptor agonist (MABA). β2AR/M-receptor agonist-1 shows potency to β2 adrenoceptor with an EC50 value of 9.2 nM. β2AR/M-receptor agonist-1 also has potency to muscarinic receptor with a Ki value of 30.2 nM. β2AR/M-receptor agonist-1 shows MABA potency with an EC50 value of 4.0 nM[1].