α2-adrenoceptor

Ritanserin (R 55667) is a highly effective, relatively selective, long-acting 5-HT2 receptor antagonist (IC50: 0.9 nM), with less activity on Histamine H1, Dopamine D2, Adrenergic α1, and Adrenergic α2 receptors.

Dexmedetomidine hydrochloride (Precedex) is an imidazole derivative that is an agonist of the adrenergic alpha-2 receptor. It is closely-related to MEDETOMIDINE, which is the racemic form of this compound.

Mirtazapine (6-Azamianserin) is a tetracyclic antidepressant with a somewhat unique mechanism of action. Mirtazapine therapy can be associated with transient asymptomatic elevations in serum aminotransferase levels and has been linked to rare instances of clinically apparent acute liver injury.

Dexmedetomidine is a Central alpha-2 Adrenergic Agonist. The mechanism of action of dexmedetomidine is as an Adrenergic alpha2-Agonist. The physiologic effect of dexmedetomidine is by means of General Anesthesia.

Medetomidine hydrochloride (MPV785) is a selective α2-adrenoceptor agonist, with Ki of 1.08 nM, exhibts 1620-fold selectivity over α1-adrenoceptor.

Clonidine hydrochloride (Catapres) is a centrally active α-adrenergic agonist used predominantly as an antihypertensive agent.

1-(2-Pyridyl)piperazine (NSC-13778) is a selective α2-adrenoceptor antagonists. 1-(2-Pyridyl)piperazine shows sympatholytic activity. 1-(2-Pyridyl)piperazine is also a metabolite of Azaperone.

Atipamezole is a synthetic α2 adrenergic receptor antagonist. It has also been researched in humans as a potential anti-Parkinsonian drug. Atipamezole hydrochloride (MPV-1248 hydrochloride) is hydrochloride form of atipamezole.

N-methyltyramine is an alkaloid isolated from the leguminous plant Acacia grandiflora.It is an α2-adrenoceptor antagonist that regulates adrenergic receptors through enzymatic adrenergic synthesis.It is used in the study of intestinal disorders.N-methyltyramine has been used in the study of intestinal disorders.N-methyltyramine has been used in the study of intestinal disorders.

Fluparoxan hydrochloride is a highly selective and potent α2-adrenoceptor antagonist for the prevention, amelioration or treatment of neurodevelopmental disorders and neurodegenerative diseases.

Azepexole hydrochloride (4H-Oxazolo[4,5-d]azepin-2-amine, 6-ethyl-5,6,7,8-tetrahydro-, hydrochloride (1:1)) is a potent α2-Adrenoceptor agonist with anaesthetic effects.

Midaglizole ((±)-DG5128 free base, DG5128 free base) is a potent α2-adrenoceptor antagonist that acts as a hypoglycemic agent by lowering blood glucose levels and increasing blood pressure in vivo.

Midaglizole hydrochloride ((±)-DG5128) (DG5128) is a preferred α2-adrenoceptor antagonist. Midazolazole hydrochloride (DG5128) has an affinity for α2-adrenoceptor (pKi = 6.28) 7.4 times higher than that of α1-adrenoceptor.

Harmane (Loturine) is a bio-active β-Carboline and monoamine oxidase inhibitor found in coffee and tobacco smoke.

Upidosin (SB-216469) is a potential uroselective α1-adrenoceptor antagonist, α1a subtype Ki=0.34 nM, α1b subtype Ki=3.9 nM, α1d subtype Ki=1.5 nM, α2-adrenoceptor Ki=33.3 nM.

(R)-Terazosin is an active R-enantiomer of Terazosin and a potent antagonist of α1-adrenoceptor [(α1a, α1b, and α1d-adrenoceptor] with Ki values of 6.51 nM, 1.01 nM, and 1.97 nM, respectively).

Piperoxan hydrochloride (Benodaine hydrochloride) is an α2 adrenoceptor antagonist. Piperoxan (benodaine) is a drug which was the very first antihistamine to be discovered.

Guanabenz hydrochloride (NE56490) is an orally active α2-adrenoceptor agonist with hypotensive effects.

Talipexole dihydrochloride (Domnin) is a dopamine D2 receptor agonist, α2-adrenoceptor agonist, and 5-HT3 receptor antagonist in both rat cortical and intestinal membrane fractions with Ki values of 0.35 μM and 0.22 μM, respectively. It displays antiParkinsonian activity.

ST1936 (ST 1936 oxalate) is a selective and highly potent 5-HT6 receptor agonist that inhibits human 5-HT6, 5-HT7 and 5-HT2B receptors by fully activating cloned human 5-HT6 receptors. body to stimulate cAMP, Ca2+, ERK1 2 and Fyn kinase.

α2 adrenoceptor antagonist and imidazoline I1 receptor ligand

SKF 86466 hydrochloride is an α2-adrenoceptor antagonist.

Rauwolscine hydrochloride (Isoyohimbine hydrochloride) , a natural alkaloid, is a specific and reversible α2-adrenergic receptor antagonist (Ki: 12 nM) [1]. It is a stereoisomer of yohimbine, which potently antagonizes both α1- and α2-adrenergic receptors [1]. Rauwolscine hydrochloride also acts as a receptor antagonist at the serotonin 5-HT2B receptor (Ki: 14.3 nM) and as a weak partial agonist at 5-HT1A (IC50: 1.3 μM) [3]. The α2-adrenergic receptor has diverse physiological functions and antagonists like rauwolscine have numerous applications, including the modulation of mood and behavior [5].

Rilmenidine hemifumarate (S-3341 hemifumarate) is a novel, orally active and selective I1 imidazoline receptor and α2-adrenoceptor agonist that induces autophagy, regulates the proliferation of leukaemia cells, stimulates the pro-apoptotic protein Bax, and induces autophagy in human leukaemia K5 cells. induces disruption of the mitochondrial pathway and apoptosis in human leukaemia K562 cells.

Romifidine (Romifidinum) is an α2-adrenoceptor agonist with analgesic and anti-injurious properties and is used in the study of neurological disorders.

RX821002 is a potent and selective antagonist of α2-adrenoceptor with low affinity for imidazoline sites. RX821002 displays selectivity for the α2D over the α2A subtypes (pKd values are 9.7 and 8.2 respectively).

ST-91 is an agonist of α2-adrenoceptor with a mixed α-adrenergic receptor type subtype selection profile.

Fenoldopam hydrochloride is a selective D1-like dopamine receptor partial agonist. It acts as a vasodilator in vivo and does not readily cross the blood-brain barrier. Fenoldopam HCl is also an α2-adrenoceptor antagonist in vitro.

N-Methylcoclaurine (±) acts as a selective antagonist at the α2-adrenoceptor [1].

(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].

Idazoxan hydrochloride (RX 781094) is a benzodioxane-linked imidazole. It has alpha-2 adrenoceptor antagonist activity.

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.

Meranzin, a bioactive compound derived from the Traditional Chinese Medicine (TCM) Chaihu-Shugan-San (CSS) and isolated from Murraya exotica L. leaves, targets the alpha 2-adrenoceptor and engages the AMPA-ERK1/2–BDNF signaling pathway. It offers promising potential for preventing the comorbidity of atherosclerosis and depression due to its significant anti-inflammatory and analgesic properties.

Yohimbine is a nonselective alpha 2-adrenergic receptor (AR) antagonist(IC50 : 0.6 μM)

Clonidine-d4 Hydrochloride is a deuterated compound of Clonidine Hydrochloride. Clonidine Hydrochloride has a CAS number of 4205-91-8. Clonidine is a centrally active alpha-adrenergic agonist used predominantly as an antihypertensive agent, usually in combination with other agents. Despite wide scale use for many years, clonidine has not been linked definitively to either serum aminotransferase elevations or clinically apparent liver injury.

Azepexole is a selective α2-adrenoceptor agonist that exhibits greater than 300-fold selectivity for the α2-adrenoceptor over the α1-adrenoceptor.

Fipamezole HCl, a α2-adrenoceptor antagonist, is used potentially for the treatment of dyskinesia associated with Parkinson's disease.

Guanoxabenz (Hydroxyguanabenz) hydrochloride is an α2 adrenergic receptor agonist with a Ki of 4000 nM and a fully activated form of 40 nM for the α2A adrenoceptor[1][2][3].

Imiloxan hydrochloride is an α2-adrenoceptor antagonist.

Atipamezole (Antisedan) is a synthetic α2 adrenergic receptor antagonist. It has also been researched in humans as a potential anti-Parkinsonian drug.

Tetrahydroalstonine is an indole alkaloid extracted from the fruit of Rhazya stricta and is a selective α2-adrenoceptor antagonist. tetrahydroalstonine has shown antipsychotic activity in Rauwolfia tetraphylla.

Clonidine (Kapvay) is a centrally active alpha-adrenergic agonist used predominantly as an antihypertensive agent, usually in combination with other agents. Despite wide-scale use for many years, clonidine has not been linked definitively to either serum aminotransferase elevations or clinically apparent liver injury.