Doxazosin mesylate(UK 33274) is a quinazoline-derivative that selectively antagonizes postsynaptic α1-adrenergic receptors.Target: α1-adrenergic receptorDoxazosin (mesylate) is the mesylate salt form of doxazosin, which is a long-lasting inhibitor of α1-adrenoceptors that is widely used to treat benign prostatic hyperplasia and lower urinary tract symptoms [1]. doxazosin may have a direct inhibitory effect on cholesterol synthesis independent of the LDL receptor. The inhibition of cholesterol synthesis by doxazosin may cause cells to compensate by upregulating the LDL receptor, thereby increasing the importation of lipoprotein cholesterol and reducing LDL cholesterol in the medium [2]. Doxazosin monotherapy was effective in eight of 12 patients (66.7%), and combined therapy with a beta-blocker was effective in 11 of 12 patients (91.7%). The mean pulse rate remained constant throughout therapy. Adverse reactions were minor and transient and occurred in only three patients. Urinary and plasma catecholamine levels tended to decrease or remained unchanged during doxazosin therapy [3].
Betaxolol Hydrochloride is a selective beta1 adrenergic receptor blocker used in the treatment of hypertension and glaucoma.Target: Beta1 Adrenergic ReceptorBetaxolol is a cardioselective beta-adrenergic receptor blocking agent. Betaxolol (5 mg/kg via i.p. injection) was administered at 24 and then 44 h following the final chronic cocaine administration. Animals treated with betaxolol during cocaine withdrawal exhibited a significant attenuation of anxiety-like behavior characterized by increased time spent in the open arms and increased entries into the open arms compared to animals treated with only saline during cocaine withdrawal. Betaxolol did not produce anxiolytic-like effects in control animals treated chronically with saline [1]. Betaxolol produces less systemic beta 2- and possibly beta 1-adrenergic receptor blockade than either timolol or levobunolol. Betaxolol may be relatively safer to use in patients with reactive airway disease than either timolol or levobunolol [2].
Latrepirdine dihydrochloride is a neuroactive compound with antagonist activity at histaminergic, α-adrenergic, and serotonergic receptors. Latrepirdine stimulates amyloid precursor protein (APP) catabolism and amyloid-β (Aβ) secretion.
Medetomidine Hydrochloride is an agonist of adrenergic alpha-2 receptor, which is used in veterinary medicine for its analgesic and sedative properties.Target: Adrenergic alpha-2 ReceptorMedetomidine, acting at alpha(2A) adrenoceptors, must be present during the encoding process to decrease discrete cue fear memory; however, its ability to suppress contextual memory is likely the result of blocking the consolidation process [1]. Medetomidine had no analgesic effects in alpha(2A)-adrenoceptor KO mice [2]. Medetomidine was effective in blocking these sympathomimetic actions of cocaine even in all 7 subjects who were homozygous for the Del322-325 polymorphism in the alpha2C AR, a loss-of-function mutation that is highly enriched in blacks [3].
Fenoterol is a β 2 adrenergic agonist designed to open up the airways to the lungs, is classed as sympathomimetic β2 agonist and asthma medication.
α1 adrenoceptor-MO-1, an S enantiomer, has affinity at alpha 1 adrenergic receptor, shows alphalytic activity, and possesses analgesic action; more active than R enantiomer.
Phentolamine-d4 (Phentolamine-d4) hydrochloride is the deuterium labeled Phentolamine hydrochloride. Phentolamine hydrochloride is a reversible, non-selective, and orally active blocker of α1 and α2 adrenergic receptor that expands blood vessels to reduce peripheral vascular resistance. Phentolamine hydrochloride can be used for the research of pheochromocytoma-related hypertension, heart failure and erectile dysfunction[1][2][3].
Tasipimidine sulfate is an orally active and selective α2A-adrenoceptor agonist with a pEC50 of 7.57 against human α2A-adrenoceptor. Tasipimidine sulfate can be used for situational anxiety and fear research[1].
Falintolol, (Z)-, a new β-adrenergic antagonist, is characterized by the presence of an oxime function.
Terbutaline sulfate is a β2-adrenergic receptor agonist; a fast-acting bronchodilator and a tocolytic to delay premature labor.
Lofexidine is a selective α2-receptor agonist, commonly used to alleviate the physical symptoms of heroin and other types of opioid withdrawal[1][2].
Tulobuterol hydrochloride is a β2-adrenoceptor agonist.
Salbutamol-d9 (acetate) is the deuterium labeled Salbutamol[1]. Salbutamol is a short-acting β2-adrenergic receptor agonist used for the relief of bronchospasm in conditions such as asthma and chronic obstructive pulmonary disease (COPD).
Rotigotine Hydrochloride is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Ki of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
UK 14,304 is a full α2-adrenergic receptor (α2-AR) agonist.Target: α2-adrenergic Receptor[3H]UK 14,034 is a full agonist at alpha 2-adrenergic receptors. [3H]UK 14,304 labels at least 2 specific binding sites in human brain that both have the characteristics of an alpha 2-adrenergic binding site. GTP decreases agonist binding at both of these sites, but with different potencies at each site [1-3].
Isoprenaline hemisulfate is a non-selective β-adrenergic receptor agonist with potent peripheral vasodilator, bronchodilator, and cardiac stimulating activities[1][2][3][4][5].
Clozapine-d4 (HF 1854-d4) is the deuterium labeled Clozapine. Clozapine is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors[1][2][3][4][5].
Sertindole-d4 (Lu 23-174-d4) is the deuterium labeled Sertindole. Sertindole, a neuroleptic, is one of the newer antipsychotic medications available[1][2].
Ivabradine (hydrochloride) is a new If inhibitor with IC50 of 2.9 μM, and used as a pure heart rate lowering agent.
(Rac)-Timolol-d5 Maleate ((Rac)-L-714,465-d5 Maleate) is a labelled racemic (S)-Timolol maleate. (S)-Timolol Maleate (L-714,465 Maleate) is a non-cardioselective hydrophilic β-adrenoceptor blocker. (S)-Timolol Maleate is widely used as standard medication for intraocular pressure (glaucoma) by preventing the production of aqueous humor. (S)-Timolol Maleate can be used for hypertension, angina pectoris and myocardial infarction[1][2][3].
Vemtoberant is an β3 Adrenergic Receptor antagonist. Vemtoberant can be used for research of β3 adrenergic receptor-mediated disorder, such as, heart failure[1][2].
2',5'-Dideoxyadenosine is a potent and non-competitive adenylyl cyclase inhibitor via binding the P-site with an IC50 of 3 µM . 2',5'-Dideoxyadenosine is a nucleoside analog and exerts a potent antiadrenergic action in heart[1][2].
Adrenalone hydrochloride is a selective α1-adrenoceptor agonist, used as a topical vasoconstrictor and hemostatic, used to prolong the action of local anesthetics.
ZD-7114 hydrochloride is a potent and selective agonist of β3-adrenergic. ZD-7114 hydrochloride is a selective thermogenic agent in vivo. ZD-7114 hydrochloride can be used in study obesity and diabetes[1].
Upidosin (Rec 15/2739) is an α-1 adrenoceptor (α-1 AR) antagonist. Upidosin shows moderate selectivity for the α-1A AR subtype. Upidosin shows uroselectivity in urethra and prostate with a Kb value of 2-3 nM higher than in ear artery and aorta with a Kb value of 20-100 nM. Upidosin inhibits [3H]prazosin binding to cloned human α-1A adrenergic receptor. Upidosin can be used for the research of urethral obstruction[1].
Vilanterol trifenatate is a long-acting β2-adrenoceptor (β2-AR) agonist with inherent 24-hour activity. The pEC50s for β2-AR, β1-AR and β3-AR are 10.37, 6.98 and 7.36, respectively.
β2AR/M-receptor agonist-2 (compound 15) is a muscarinic antagonist and β2 adrenoceptor agonist (MABA). β2AR/M-receptor agonist-2 shows potency to β2 adrenoceptor with an EC50 value of 3.7 nM. β2AR/M-receptor agonist-2 also has potency to human cloned M3 receptor with a Ki value of 0.73 nM. β2AR/M-receptor agonist-2 is a potent bronchodilator, it can be used for the research of chronic obstructive pulmonary disease (COPD)[1].
Alfuzosin 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.
CGP 12177 ((±)-CGP 12177) hydrochloride is a β Adrenergic Receptor Ligand. CGP 12177 hydrochloride is a high affinity antagonist of β1- and β2-AR. CGP 12177 hydrochloride is also shown to interact, with a lower affinity, with the β3-AR and to exhibit a partial agonist activity on rodent and human β3-AR. CGP 12177 hydrochloride exhibits partial agonist properties for α1-AR in rat pulmonary artery[1].
Clozapine D8 (HF 1854 D8) is the deuterium labeled Clozapine. Clozapine, an antipsychotic, is a potent antagonist of dopamine and a number of other receptors, with a Ki of 9.5 nM for muscarinic M1 receptor. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM)[1][2][3][4].