Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells[1][2][3].
Bambuterol Hcl is a long acting beta-adrenoceptor agonist (LABA) used in the treatment of asthma; it also is a prodrug of terbutaline.IC50 value:Target: beta-adrenoceptor agonistBambuterol is contraindicated in pregnancy and in people with seriously impaired liver function. It can be used by people with renal impairment, but dose adjustments are necessary. The adverse effect profile of bambuterol is similar to that of salbutamol, and may include fatigue, nausea, palpitations, headache, dizziness and tremor.
Methoxamine hydrochloride is a noradrenergic α1 agonistsup>[1].
β2AR agonist 3 (compound 9a) is a β2-adrenergic receptor (β2AR) agonist. β2AR agonist 3 can be used for type 2 diabetes research[1].
Oxprenolol (Ba 39089 free base) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a Ki of 7.10 nM in a radioligand binding assay using rat heart muscle[1].
Glaucine (O,O-Dimethylisoboldine) is an alkaloid isolated from Glaucium flavum Crantz with antitussive, bronchodilation and anti-inflammatory properties. Glaucine is a selective and orally active phosphodiesterase 4 (PDE4) inhibitor with Kis of 3.4 µM in human bronchus and polymorphonuclear leukocytes. Glaucine is also a non-selective α-adrenoceptor antagonist, a Ca2+ entry blocker, and a weak dopamine D1 and D2 receptor antagonist. Glaucine has antioxidative and antiviral activities[1][2][3].
Carteolol is a non-selective β-adrenoceptor antagonist. Carteolol induces apoptosis via a caspase activated and mitochondrial-dependent pathway. Carteolol can be used for glaucoma research[1].
Rauwolscine is a selective α2-adrenoceptor antagonist that inhibits tumor growth and induces apoptosis[1].
Methyl maslinate is a β-adrenergic antagonist. Methyl maslinate is a potent cardiotonic and antidysrhythmic agent. Methyl maslinate has the potential for hypertension research[1].
(R)-(-)-Phenylephrine is a selective α1-adrenoceptor agonist primarily used as a decongestant.
Alloyohimbine, an alkaloid, is a selective α2-adrenoceptor antagonist with K Dα1, K Dα2 of 0.28 μM and 0.006 μM, respectively[1].
Formoterol fumarate(Foradil) is a potent, selective and long-acting β2-adrenoceptor agonist.IC50 Value: 2.1 nM in pregnant C3H/HeN strain mice[5]Target: β2 receptorBudesonide/formoterol in a single inhaler for both maintenance and reliever therapy is now an established therapeutic option for management of inadequately controlled asthma[4].in vitro:. The long-acting β(2)-agonist formoterol and the glucocorticoid dexamethasone significantly reduced HRV-induced ERK phosphorylation, Fra-1, and MMP-9 expression in BEAS-2B cells[3].in vivo: compared the bronchodilatory effects of inhaled budesonide/formoterol (dose: 200 μg and 12 μg respectively) combination with budesonide (200 μg)/salbutamol (200 μg) administered by metered dose inhaler and spacer in children of 5-15 years with mild acute exacerbation of asthma [Modified Pulmonary Index Score (MPIS) between 6-8] in this double-blind, randomized controlled trial. The primary outcome was FEV1 (% predicted) in the two groups at 1, 5, 15, 30, 60 min after administration of the study drug[1]. Fifteen randomized, placebo-controlled clinical trials including COPD patients were evaluated: indacaterol 75 μg once daily (n = 2 studies), indacaterol 150 μg once daily (n = 5), indacaterol 300 μg once daily (n = 4), FOR/BUD 9/160 μg twice daily (n = 2), FOR/BUD 9/320 μg twice daily (n = 2), SAL/FP 50/500 μg twice daily (n = 4), and SAL/FP 50/250 μg twice daily (n = 1)[2].Clinical trial: Effects of Mometasone Furoate/Formoterol Combination Versus Mometasone Furoate Alone in Persistent Asthmatics (Study P04073) . Phage3
ICI141292 is a potent β-adrenoceptor partial agonist with a greater affinity for β1- than β2-adrenoceptors.
Hydroxybupropion is the major active metabolite of Bupropion. Hydroxybupropion is metabolized by CYP2B6.Bupropion is an atypical antidepressant and smoking-cessation agent. Hydroxybupropion inhibits norepinephrine uptake with an IC50 value of 1.7 μM. Hydroxybupropion is also a nACh receptor antagonis tis more potent than Bupropion[1] .
DL-Epinephrine is the racemate of epinephrine. L-Epinephrine is a hormone secreted by the medulla of the adrenal glands. L-Epinephrine is an α-adrenergic and β-adrenergic receptor agonist.
Benzquinamide is an antiemetic which can bind to the α2A, α2B, and α2C adrenergic receptors (α2-AR) with Ki values of 1,365, 691, and 545 nM, respectively.
Dexmedetomidine 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 ReceptorDexmedetomidine, 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]. Dexmedetomidine had no analgesic effects in alpha(2A)-adrenoceptor KO mice [2]. Dexmedetomidine 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].
ST1936 is a selective, nanomolar affinity 5-HT6 receptor agonist with Ki values of 13 nM, 168 nM and 245 nM for human 5-HT6, 5-HT7 and 5-HT2B receptors, respectively. ST1936 also shows moderate affinity (Ki of 300 nM) for human and rat α2 adrenergic receptor[1].
Fiduxosin is a potent α1-adrenoceptor antagonist, with Ki of 0.160 nM, 24.9 nM, and 0.920 nM for α1a-, α1b-, and α1d-adrenoceptors, respectively.
Etilefrine hydrochloride is an orally active α adrenergic agonist. Etilefrine hydrochloride is also an AMPK activator. Etilefrine hydrochloride can be used for the research of postural hypotension[1][2][3][4].
AVN-101 hydrochloride is a potent, brain-penetrant and orally active 5-HT7 receptor antagonist (Ki of 153 pM), with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors (Ki values of 2.04 nM, 1.56 nM, and 1.17 nM, respectively). AVN-101 hydrochloride also exhibits a rather high affinity toward histamine H1 (Ki of 0.58 nM) and adrenergic α2A, α2B, and α2C (Ki= 0.41-3.6 nM) receptors. AVN-101 hydrochloride can be studied in such diseases as general anxiety disorders, depression, schizophrenia, and multiple sclerosis[1].
Pindolol (LB-46) is a nonselective β-blocker with partial beta-adrenergic receptor agonist activity, also functions as a 5-HT1A receptor weak partial agonist / antagonist (Ki=33nM).
A-123189 is a selective and potent α1D antagonist with Kis of 0.312 and 0.17 for human α1D and rat α1D, respectively. A-123189 displays selectivities between 10- to 20-fold for the α1D receptor over the human α1A and rat α1A receptors[1].
SB-206606, a stereoisomer of BRL 37344, is a potentially specific, beta 3-adrenergic receptor (β3-AR) ligand. The affinity of [3H]SB 206606 is 76 times higher for the β3-AR than for the beta 1/beta 2-adrenergic receptors[1].
L-(-)-α-Methyldopa hydrochloride 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.
5-Methylurapidil isα1A‐adrenoceptor antagonist. 5-Methylurapidil can be used for the research of cardiovascular diseases such as hypertension and heart failure[1].
Indoramin is an orally active antihypertensive agent. Indoramin is also selective for the α1A-adrenoceptor[1].
Lidanserin is a drug which acts as a combined 5-HT2A and α1-adrenergic receptor antagonist.
Benoxathian hydrochloride is a potent α1 adrenoceptor antagonist, can be used for researching anorexia[1].
Levobetaxolol is a potent and high affinity β-adrenergic antagonist with IC50 values of 33.2, 2970, 709 nM for guinea pig atrial β1, tracheal β2 and rat colonic β3 receptors, respectively. Levobetaxolol reduces IOP (intraocular pressure). Levobetaxolol exhibits a micromolar affinity for L-type Ca21-channels. Levobetaxolol decreases the effects of ischaemia/reperfusion injury in rats. Levobetaxolol has the potential for the research of glaucoma[1][2].