G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
Sulfinalol is an orally active β-adrenoceptor antagonist with direct vasodilator activity[1].
Broxaterol (Z 1170) is the an agonist of β2 adrenergic receptor that affects the smooth muscle receptors in the body. Broxaterol plays an important role in respiratory disease[1].
Spirendolol is a β adrenergic receptor antagonist.
Silodosin (Rapaflo; KMD-3213) is an α1-adrenoceptor antagonist with high uroselectivity; In treatment of dysuria.IC50 Value:Target: Adrenergic Receptorin vitro: Silodosin potently inhibited 2-[2-(4-hydroxy-3-[125I]iodophenyl)ethylaminomethyl]-alpha-tetralone binding to the cloned human alpha 1a-AR, with a Ki value of 0.036 nM, but had 583- and 56-fold lower potency at the alpha 1b- and alpha 1d-ARs, respectively. Silodosin inhibited norepinephrine-induced increases in intracellular Ca2+ concentrations in alpha 1a-AR-expressing Chinese hamster ovary cells with an IC50 of 0.32 nM but had a much weaker inhibitory effect on the alpha 1b- and alpha 1d-ARs.in vivo: Using pharmacologically well characterized native rat tissues [submaxillary gland (alpha 1A-AR-expressing tissue), liver (alpha 1B-AR-expressing tissue), and heart (mixed alpha 1A- and alpha 1B-AR-expressing tissue)], binding studies showed that inhibition curves for Silodosin in submaxillary gland and liver best fit a one-site model (with Ki values of 0.15 and 16 nM, respectively), whereas Silodosin had high and low affinity sites in heart membranes. Chloroethylclonidine treatment of rat heart membranes completely eliminated the low affinity sites for Silodosin. Furthermore, in human liver and prostate Silodosin could identify high and low affinity sites, the Ki values of which corresponded well to those for the cloned human alpha 1a- and alpha 1b-ARs, respectively. Moreover, the affinity of Silodosin was found to be approximately 10-fold higher at the cloned human alpha 1a-AR than at the cloned rat alpha 1a-AR.v
Metoprolol (Toprol) is a selective β1 receptor blocker used in treatment of several diseases of the cardiovascular system, especially hypertension.IC50 value:Target: β1 receptor
(Rac)-Rotigotine (N-0437) is a racemate of Rotigotine. Rotigotine is a full agonist of?dopamine receptor, a partial agonist of the?5-HT1A receptor, and an antagonist of the?α2B-adrenergic receptor, with?Kis of 0.71?nM, 4-15?nM, and 83?nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
Vemtoberant mesylate is an β3 Adrenergic Receptor antagonist. Vemtoberant mesylate can be used for research of β3 adrenergic receptor-mediated disorder, such as, heart failure[1][2].
Mebeverine metabolite O-desmethyl Mebeverine alcohol is a metabolite of Mebeverine, which is a potent α1 repector inhibitor, causing relaxation of the gastrointestinal tract.
SR59230A is a potent, selective, and blood-brain barrier penetrating β3-adrenergic receptor antagonist[1] with IC50s of 40, 408, and 648 nM for β3, β1, and β2 receptors, respectively[2].
Dexmedetomidine ((+)-Medetomidine) is a potent, selective and orally active agonist of α2-adrenoceptor, with a Ki of 1.08 nM. Dexmedetomidine shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine exhibits anxiolysis, sedation, and modest analgesia effects[1][2][3].
OPC-28326 is a selective peripheral vasodilator and an angatonist of α2-adrenergic receptor, with Ki of 2040, 285, and 55 nM for α2A-, α2B- and α2C-adrenoceptors, respectively.
Detomidine carboxylic acid is the major urinary metabolite of Detomidine. Detomidine is a synthetic α2-adrenergic agonist and an animal analgesic sedative. Detomidine also has cardiac and respiratory effects and an antidiuretic action[1][2].
Amosulalol (YM 09538) is an orally active and dual inhibitor of α1/β1-Adrenergic Receptor. Amosulalol exhibits antihypertensive activity via α1-Adrenergic Receptor inhibition. Amosulalol decreases reflexogenic increases in heart rate and plasma renin activity (PRA) via β1-Adrenergic Receptor inhibition in spontaneously hypertensive rats (SHR)[1].
(E)-Guanabenz ((E)-Wy-8678) is an orally active central α2-adrenoceptor agonist. (E)-Guanabenz has antihypertensive activity, acts via stimulating central α2-adrenoceptors, and reducing net sympathetic outflow into the periphery. (E)-Guanabenz also directly binds to and inhibits GADD34, and has neuroprotective activity. (E)-Guanabenz can be used for researching hypertension and Parkinson disease[1][2].
Carvedilol-d5 is deuterium labeled Carvedilol. Carvedilol (BM 14190) is a non-selective β/α-1 blocker[1]. Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure[2]. Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome[3].
Carvedilol is a non-selective beta blocker/alpha-1 blocker with an IC50 of 3.8 μM for inhibition of LDL oxidation.IC50 Value: 3.8 μM ( inhibition of LDL oxidation)Target: beta Adrenergic ReceptorCarvedilol is a nonselective-blocking agent and is used in the treatment of hypertension and angina pectoris. As a third-generation β-adrenergic blocker (β-blocker), Carvedilol is able to reverse cardiac structural remodeling. Recentresults demonstrated that the effect caused by Carvedilol on cardiac remodeling is largely dependent on endogenous NO.
Phenoxybenzamine-d5 is the deuterium labeled Phenoxybenzamine[1]. Phenoxybenzamine is a nonselective, irreversible, orally active α-adrenoceptor antagonist that is commonly used for the research of hypertension, specifically caused by pheochromocytoma. Phenoxybenzamine also shows antitumor activity[2][3].
Agroclavine is a natural, clavine type of ergot alkaloid. Agroclavine is a D1 dopamine receptor and α1-adrenoceptor agonist. Agroclavine also has anticancer and antimicrobial activities[1][2].
Vatinoxan hydrochloride (MK-467 hydrochloride;L-659066 hydrochloride) is a peripheral α2 adrenergic receptor antagonist.
ARC 239 is an α2B/C-adrenergic receptor antagonist with pKi of 7.06 and 6.95 for rat kidney α2B and human α2C, respectively. ARC 239 also inhibits 5-HT1A receptor with a Ki of 63.1 nM[1][2].
Tetrahydroalstonine, a indole alkaloid isolated from the fruits of Rhazya stricta, is a selective alpha 2-adrenoceptor antagonist[1][2].
Acebutolol is an orally active β1 adrenergic receptor (β1AR) antagonist. Acebutolol is used for hypertension, angina pectoris and cardiac arrhythmias research[1][2][3].
Olodaterol (BI1744) hydrochloride is a selective, long acting β2-adrenoceptor (β2-AR) agonist (EC50=0.1 nM and pKi= 9.14 for human β2-adrenoceptor, respectively). Olodaterol can be used for chronic obstructive pulmonary disease (COPD) and pulmonary fibrosis[1][2][3].
Mezilamine is a potent antidopaminergic agent. Mezilamine induces a concentration dependent increase in the electrically stimulated overflow of 3H-noradrenaline from rat cortical slices, without affecting the basal overflow. Mezilamine acts as a presynaptic α-adrenoceptor antagonist and a postsynaptic α-adrenoceptor agonist[1].
Zotepine, an antipsychotic agent, is a potent antagonist of 5-HT2A, 5-HT2C, Histamine H1, α1-adrenergic and Dopamine D2 receptors, with Kds of 2.6 nM, 3.2 nM, 3.3 nM, 7.3 nM and 8 nM, respectively. Zotepine exhibits antidepressive and anxiolytic effects in vivo[1][2].
Xylazine is α2 class of adrenergic receptor agonist.Target: Adrenergic ReceptorXylazine is a drug that is used for sedation, anesthesia, muscle relaxation, and analgesia in animals such as horses, cattle and other non-human mammals. An analogue of clonidine, it is an agonist at the α2 class of adrenergic receptor. Xylazine has recently emerged as a recreational drug, especially in Puerto Rico [1]. Administration of xylazine (0.17 mg/kg of body weight, diluted to a 10-ml volume, using 0.9% NaCl) induced approximately 2.5 hours of local analgesia without apparent side effects. Higher doses of xylazine caused mild hind limb ataxia. Administration of lidocaine induced a similar duration of analgesia, with severe hind limb ataxia (100% incidence). We concluded that xylazine given by epidural injection results in safe, effective perineal analgesia in horses [2].
Prazosin is an alpha-adrenergic blocker and is a sympatholytic drug used to treat high blood pressure and anxiety, PTSD, and panic disorder.Target: Adrenergic ReceptorPrazosin, is a sympatholytic drug used to treat high blood pressure and anxiety, PTSD, andpanic disorder. It is an alpha-adrenergic blocker that is specific for the alpha-1 receptors. These receptors are found on vascular smooth muscle, where they are responsible for the vasoconstrictive action of norepinephrine. They are also found throughout the central nervous system. As of 2013, prazosin is off-patent in the US, and the FDA has approved at least one generic manufacturer.In addition to its alpha-blocking activity, prazosin is an antagonist of the MT3 receptor (which is not present in humans), with selectivity for this receptor over the MT1 and MT2 receptors.Prazosin is orally active and has a minimal effect on cardiac function due to its alpha-1 receptor selectivity. However, when prazosin is initially started, heart rate and contractility go up in order to maintain the pre-treatment blood pressures because the body has reached homeostasis at its abnormally high blood pressure. The blood pressure lowering effect becomes apparent when prazosin is taken for longer periods of time. The heart rate and contractility go back down over time and blood pressure decreases.
Tamsulosin is a selective α1 receptor antagonist.Target: α1 receptorTamsulosin is a selective α1 receptor antagonist that has preferential selectivity for the α1A receptor in the prostate versus the α1B receptor in the blood vessels. Tamsulosin-treated patients had a 0.30-fold lower risk of developing acute urinary retention compared with control patients. None of the International Continence Society male questionnaire domain scores showed significant changes between the groups [1]. tamsulosin can be recommended for treating men after catheterization for AUR, and can reduce the likelihood of the need for re-catheterization [2].
Etilefrine (3-[2-(ethylamino)-1-hydroxyethyl]phenol) is an α adrenergic agonist[2]. Etilefrine also is an AMPK activator[1]. Etilefrine can be used for the research of postural hypotension[3].