adrenoceptors

Sarpogrelate hydrochloride (MCI-9042) , a selective 5-HT2 antagonist, has been widely used as an anti-platelet agent for the treatment of PAD. Target: 5-HT2 Recepter Sarpogrelate is a drug which acts as an antagonist at the 5HT2A and 5-HT2B receptors. Sarpogrelate hydrochloride was shown to have the same affinity as ritanserin for 5-HT2A receptors, with a Ki value of 8.39 nM. Sarpogrelate hydrochloride lacked prominent 5-HT1-like, 5-HT3, beta, H1, H2 and M3 antagonist activity and weakly blocked alpha 1-adrenoceptors (pKB = 6.30). (S)-M-1 showed weak affinity for 5-HT1-like receptors (pKB = 6.30), alpha 1- (pKB = 6.80) and beta- (pKB = 6.54) adrenoceptors, while (R)-M-1 was a weak antagonist at histamine H1 receptors (pKB = 6.49). After 12 weeks of sarpogrelate administration, FBF and LBF responses during RH showed significant increases from 13.2 +/- 1.7 to 18.1 +/- 2.2 mL/min per 100 mL tissue (P < 0.01) and from 8.2 +/- 0.9 to 14.2 +/- 2.1 mL/min per 100 mL tissue (P < 0.05), respectively. Sarpogrelate hydrochloride -induced augmentation of FBF and LBF responses to RH was maintained at 24 weeks. Long-term oral administration of sarpogrelate improves vascular function in patients with PAD.

Higenamine hydrochloride (norcoclaurine HCl) has been demonstrated to be a β2 adrenoreceptor agonist. Adrenergic receptors, or adrenoceptors, belong to the class of G protein–coupled receptors, and are the most prominent receptors in the adipose membrane, besides also being expressed in skeletal muscle tissue.

OPC-28326 is a specific an α2-adrenergic receptor antagonist and acts as a peripheral vasodilator. OPC-28326 inhibits α2A-, α2B- and α2C-adrenoceptors with Ki of 2040, 285, and 55 nM, respectively.

T-0509 is a selective beta 1 receptor agonist that increases inotropy in canine ventricular muscle and selectively down-regulates rat cardiac beta 1-adrenoceptors.

L-745870 trihydrochloride is a highly potent and selective D4 dopamine receptor antagonist.

(±)-Tazifylline is a selective and long-acting antagonist of histamine H1 receptor. Tazifylline shows much lower affinity for H2 receptors, α- and β-adrenoceptors, 5-hydroxytryptamine and muscarinic receptor subtypes.

1. Dihydrolycorine-HCL(DL) shows hypotensive effects, it can block alpha 1-adrenoceptors. 2. Dihydrolycorine is an inhibitors of protein synthesis in eukarytic cells, it halts protein synthesis in eukaryotic cells by inhibiting the peptide bone formation

L-Albizziin (2-Methoxyidazoxan monohydrochloride) is a highly potent selective antagonist of the alpha 2r adrenergic receptor, with little or no antagonistic effect on imidazoline. It has a significantly higher affinity for the alpha 2D adrenergic receptor (pKd9.7) in guinea pigs than for the alpha 2A adrenergic receptor (pKd8.2) in rabbits.

BU 226 hydrochloride demonstrates affinity for imidazoline (I) receptors, in particular the I2 binding site with a Ki of 1.4 nM. BU 226 hydrochloride showed low (microM) affinity for alpha 2-adrenoceptors.

Adenosine A1 receptor activator T62 is an allosteric enhancer of the adenosine A1 receptor, producing antinociception in animal models of acute pain and reducing hypersensitivity in models of inflammatory and nerve-injury pain[1][2][3].

FG 7142 (LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50= 137 nM). FG 7142 can increase tyrosine hydroxylation and cause upregulation of β-adrenoceptors in mouse cerebral cortex. FG 7142 , a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (Ki=91 nM).

Alprenolol-nbd is a fluorescent beta-adrenoceptor probe that binds irreversibly to beta-adrenoceptors and non-receptor binding sites.

Delequamine HCl is a potent and selective alpha 2-adrenoceptor antagonist. Delequamine HCl has a pKi of 9.45 for alpha 2-adrenoceptors in the rat cortex (pA2 in the guinea-pig ileum of 9.72).

Trifolirhizin exerts varying degrees of inhibition on tyrosinase-dependent melanin biosynthesis, and therefore, are candidates as skin-whitening agents.Trifolirhizin possesses potential anti-inflammatory and anti-cancer activities.Trifolirhizin shows in vitro inhibitory effects on the growth of human A2780 ovarian and H23 lung cancer cells. Trifolirhizin inhibits acetylcholine mediated airway smooth muscle (ASM) contraction or directly relaxes pre-contracted ASM independent of β 2 -adrenoceptors.

Nantenine is an acetylcholinesterase inhibitor, it functions as an effective antagonist against a wide range of MDMA-induced effects in mice. Nantenine has anticonvulsant effect, which seems attributable to its stimulation and the resultant decrease of Ca

BFE-55 is derivative of befunolol (a beta-adrenergic partial agonist). BFE-55 interacts with only the high affinity sites in beta-adrenoceptors

BFE-61 is a partial agonist of the beta-adrenoceptors.

DJ 7141 is a unique alpha-2 agonist which shows high affinity to peripheral alpha-2 adrenoceptors but only a mild hypotensive activity.

Mezilamine is an antagonist of dopamine. It also blocks presynaptic but stimulating postsynaptic alpha-adrenoceptors.

Mabuterol hydrochloride is a selective β2 adrenoreceptor agonist. Mabuterol has a specific effect on beta 2-adrenoceptors with no beta 1-stimulation.

Doxazosin (UK 33274) is a long-acting α1-adrenoceptor inhibitor widely used to treat benign prostatic hyperplasia and lower urinary tract symptoms.

L748337 is a competitive and potent β3-adrenoceptor antagonist that inhibits the action of β3-, β2-, and β1-adrenoceptors, activates MAPK signaling, promotes phosphorylation of Erk1/2, and inhibits the protective effects of CL316243, and is used in the study of disorders caused by abnormalities of the β3-adrenoceptors.

Fadolmidine, also known as MPV-2426, is a novel and potent alpha2 -adrenoceptor (alpha2) -AR) agonist developed for spinal analgesia. Fadolmidine displayed high affinity and full agonist efficacy at all three human alpha2-adrenoceptor subtypes (A, B and C) in transfected CHO cells with EC50 values (nM) of 0.4, 4.9 and 0.5, respectively. Fadolmidine inhibited also electrically evoked contractions in rat vas deferens demonstrating the activation of rodent presynaptic alpha2D-adrenoceptors with an EC50 value of 6.4 nM. Moreover, fadolmidine was a full agonist at human alpha1A-adrenoreceptor (EC50 value 22 nM) and alpha1B-adrenoreceptor (EC50 value 3.4 nM) in human LNCaP cells and transfected HEK cells, respectively. Agonism at the alpha1-adrenoceptor was also observed in rat vas deferens preparations although at lower potency (EC50 value 5.6 microM). Fadolmidine demonstrated potent alpha2-adrenoceptor agonist activity also in vivo by inhibiting electrically induced tachycardia i......

The alpha-adrenoceptors blocking effect of (N-piperidinomethyl)-2-chromanne was studied in vivo and in vitro in the rat. In the pithed rat, (N-piperidinomethyl)-2-chromanne (1 mg/kg i.v.) antagonized the pressor effects induced by alpha agonists. (N-piperidinomethyl)-2-chromanne competitively antagonized the pressor effects of M7 (alpha 2-agonist) and cirazoline (alpha 1-agonist). (N-piperidinomethyl)-2-chromanne antagonized the inhibitory effects of clonidine on presynaptic alpha 2-receptors in stimulated pithed rats.

Doxazosin HCl is the salt form of Doxazosin Free Base which acts by inhibiting the postsynaptic alpha(1)-adrenoceptors on vascular smooth muscle. This inhibits the vasoconstrictor effect of circulating and locally released catecholamines (epinephrine and norepinephrine), resulting in peripheral vasodilation.

CH-38083 is a selective and effective alpha-2 adrenoceptors antagonist.

YS-49 is an activator of PI3K Akt (a downstream target of RhoA).

Epanolol is a potent β-adrenoceptor partial agonist with a greater affinity for β1- than β2-adrenoceptors.

Ulimorelin is a ghrelin receptor agonist (EC50: 29 nM and a Ki of 16 nM). Ulimorelin is a prokinetic agent and causes vasorelaxation through competitive antagonist action at α1-adrenoceptors.

(S)-Terazosin is an active S-enantiomer of Terazosin and acts as a potent, high-affinity antagonist of α-adrenoceptors [α1a, α1b, and α1d-adrenoceptors] with Ki values of 3.91 nM, 0.79 nM, and 1.16 nM, respectively.

Piribedil hydrochloride can be used in the parkinson's disease, circulatory disorders, cancers research. Piribedil hydrochloride inhibits MLL1 methyltransferase activity with EC50 value of 0.18 μM. Piribedil hydrochloride is a potent and orally active agonist of dopamine D2 and dopamine D3 as well as the antagonist of α2-adrenoceptors [1] [2] [3] [4].

(E)-Guanabenz ((E)-Wy-8678), an oral central α2-adrenoceptor agonist, exhibits antihypertensive and neuroprotective activities by stimulating central α2-adrenoceptors to reduce sympathetic outflow and directly inhibiting GADD34. It is used in researching hypertension and Parkinson's disease [1] [2].

Trimazosin is an orally active quinazoline derivative, structurally related to prazosin. trimazosin has hypotensive activity by selectively blocking alpha1-adrenoceptors.

Higenamine-d4 HCl is a deuterated compound of Higenamine HCl. Higenamine HCl has a CAS number of 11041-94-4. Higenamine(Hydrochloride) has been demonstrated to be a β2 adrenoreceptor agonist. Adrenergic receptors, or adrenoceptors, belong to the class of G protein–coupled receptors, and are the most prominent receptors in the adipose membrane, besides also being expressed in skeletal muscle tissue.

Wy 27127 is an alpha 2-adrenoceptors antagonist that has estimated potency based on ability to block clonidine-induced inhibition of electrically-evoked contractions of the rat isolated vas deferens.

Niguldipine is a calcium channel antagonist. Niguldipine shows high affinity to Ca2+ channels and to a subtype of alpha 1-adrenoceptors.

LDT3 HCl is a potent multi-target antagonists of both alpha1A- and alpha1D-adrenoceptors, and also of 5-HT1A receptors.

Chir 2279 is a N-(substituted)glycine peptoid trimer with high-affinity binding for alpha 1-adrenoceptors. CHIR 2279 antagonized the epinephrine-induced increase in intraurethal pressure (pseudo pA2, 6.86) in dogs.

Mezilamine HCl is a dopamine antagonist, blocking presynaptic but stimulating postsynaptic alpha-adrenoceptors.

Medetomidine (Domtor) is a potent, highly selective α2-adrenoceptor agonist, demonstrating Ki values of 1.08 nM for α2-adrenoceptors and 1750 nM for α1-adrenoceptors, indicating significant selectivity for α2 over α1 receptors compared to clonidine and UK 14,304 with 1620-, 220-, and 300-fold respectively. Medetomidine significantly inhibits the twitch response in electrically stimulated mouse vas deferens (pD2 = 9.0), showcasing its efficacy. Exhibiting a wide range of pharmacological effects, Medetomidine is effective in vivo, manifesting hypotensive, bradycardic, sedative, anxiolytic, hypothermic, and analgesic properties.

Moxonidine Hydrochloride serves as a selective agonist for the imidazoline receptor subtype 1 and functions as an antihypertensive agent. It primarily acts within the central nervous system and demonstrates a significant preference for I1 imidazoline receptors over α2-adrenoceptors, with a 40-fold higher affinity. This compound effectively reduces stimulated norepinephrine overflow, indicating its potent efficacy. Despite similar agents like AGN192403 targeting the same receptor, moxonidine's dose-response efficacy remains unaffected. Its ability to lower blood pressure and reduce heart rate is distinctly mediated through imidazoline receptors, reliant on well-preserved noradrenergic pathways within the rostral ventrolateral medulla (RVLM). This interaction is potentially linked to a specific 42 kDa imidazoline receptor protein, emphasizing its unique mechanism of action compared to other drugs like clonidine.

Muscarinic toxin 3 (MT3), a potent non-competitive antagonist of mAChR and adrenoceptors, exhibits pIC50 values of 6.71 for M1, 8.79 for M4, 8.86 for α1A, 7.57 for α1B, 8.13 for α1D, 8.49 for α2A, <6.5 for α2B, and 7.29 for α2C receptors. MT3 notably demonstrates significant adrenoceptor activity [1].

Substance P-related peptide that inhibits binding of G proteins to their receptors. Competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.

Bopindolol is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol is a prodrug of pindolol and can be rapidly metabolized to an active hydrolyzed form. Bopindolol can be used for essential and renovascular hypertension research [1] [2].

Sarpogrelate-d3 HCl is a deuterated compound of Sarpogrelate HCl. Sarpogrelate HCl has a CAS number of 135159-51-2. Sarpogrelate(MCI-9042) hydrochloride, a selective 5-HT2 antagonist, has been widely used as an anti-platelet agent for the treatment of PAD. Target: 5-HT2 Recepter Sarpogrelate is a drug which acts as an antagonist at the 5HT2A and 5-HT2B receptors. Sarpogrelate was shown to have the same affinity as ritanserin for 5-HT2A receptors, with a Ki value of 8.39 nM. Sarpogrelate lacked prominent 5-HT1-like, 5-HT3, beta, H1, H2 and M3 antagonist activity and weakly blocked alpha 1-adrenoceptors (pKB = 6.30). (S)-M-1 showed weak affinity for 5-HT1-like receptors (pKB = 6.30), alpha 1- (pKB = 6.80) and beta- (pKB = 6.54) adrenoceptors, while (R)-M-1 was a weak antagonist at histamine H1 receptors (pKB = 6.49). After 12 weeks of sarpogrelate administration, FBF and LBF responses during RH showed significant increases from 13.2 +/- 1.7 to 18.1 +/- 2.2 mL/min per 100 mL tissue (P < 0.01) and from 8.2 +/- 0.9 to 14.2 +/- 2.1 mL/min per 100 mL tissue (P < 0.05), respectively. Sarpogrelate-induced augmentation of FBF and LBF responses to RH was maintained at 24 weeks. Long-term oral administration of sarpogrelate improves vascular function in patients with PAD.

Wy 26392 is an alpha 2 adrenoceptors antagonist that increase central sympathetic tone and blood pressure in low doses.

ZD7114, also known as ICI-D7114, is a selective adrenoceptor agonist of brown fat and thermogenesis. ICI D7114 stimulates thermogenesis at doses that have little effect on beta 1 or beta 2 adrenoceptors. Treatment with ICI D7114 activates BAT and thermogenesis even in species and situations where the intrinsic capacity is low. ICI D7114 has beneficial effects in animal models of obesity and disturbed glucose and lipid homeostasis.

Perbufylline is a bronchodilator. It is N-methylated xanthine derivative. Perbufylline acts as a competitive antagonist at 5-HT2 and alpha1-adrenoceptors, with at least 100-fold less activity at alpha2-adrenoceptors.

Terazosin, a quinazoline derivative, is an orally active and competitive antagonist of α1-adrenoceptors. Its mechanism of action involves relaxing blood vessels and promoting bladder opening. Terazosin exhibits therapeutic potential for treating benign prostatic hyperplasia (BPH) and high blood pressure [1][2][3].

Ajmalicine (Raubasine) hydrochloride, a potent adrenolytic compound, selectively inhibits α1-adrenoceptors and acts as a reversible, non-competitive full inhibitor of nicotine receptors with an IC50 of 72.3 μM. This chemical also serves as an anti-hypertensive and exhibits sedative activity, making it useful in various therapeutic applications.