Adrenergic Receptor Beta Receptor Adrenergic receptors are a class of G protein-coupled receptors that are targets of the catecholamines, especially norepinephrine and epinephrine. Many cells possess these receptors, and the binding of a catecholamine to the receptor will generally stimulate the sympathetic nervous system. The sympathetic nervous system is responsible for the fight-or-flight response, which includes widening the pupils of the eye, mobilizing energy, and diverting blood flow from non-essential organs to skeletal muscle. There are two main groups of adrenergic receptors, α and β, with several subtypes. α receptors have the subtypes α1 and α2. β receptors have the subtypes β1, β2 and β3. All three are linked to Gs proteins, which in turn are linked to adenylate cyclase. Agonist binding thus causes a rise in the intracellular concentration of the second messenger cAMP. Downstream effectors of cAMP include cAMP-dependent protein kinase (PKA), which mediates some of the intracellular events following hormone binding. www.MedChemExpress.com 1 Adrenergic Receptor Agonists, Antagonists, Inhibitors, Activators & Modulators (+)-Penbutolol (4E)-SUN9221 ((R)-Penbutolol; (+)-Isopenbutolol) Cat. No.: HY-116790A Cat. No.: HY-U00367 (+)-Penbutolol is a β-adrenoceptor antagonist, (4E)-SUN9221 is a potent antagonist of with an IC50 of 0.74 μM. (+)-Penbutolol is an α1-adrenergic receptor and 5-HT2 receptor, with optical isomer of l-penbutolol with Na+ antihypertensive and anti-platelet aggregation channel-blocking action. activities. Purity: >95.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 1 mg, 5 mg (R)-(+)-Atenolol (R)-Carvedilol Cat. No.: HY-B2111 ((R)-BM 14190) Cat. No.: HY-B0006C (R)-(+)-Atenolol is the less active enantiomer of (R)-Carvedilol ((R)-BM 14190), the R-enantiomer of the (R,S)-atenolol. (R,S)-atenolol is a Carvedilol, is a non-selective β/α-1 blocker. β-adrenergic receptor antagonist. (R)-Carvedilol exerts protection against the vascular or cardiac toxicity of Doxorubicin (DOX). Purity: >99.0% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg Size: 1 mg, 5 mg (R)-Terazosin (Rac)-Rotigotine hydrochloride Cat. No.: HY-B0371B Cat. No.: HY-15394 (R)-Terazosin is an active R-enantiomer of (Rac)-Rotigotine hydrochloride is a racemate of Terazosin. (R)-Terazosin is a potent Rotigotine. α1-adrenoceptor antagonist with Ki values of 6.51 nM, 1.01 nM and 1.97 nM for α1a, α1b and α1d-adrenoceptor, respectively. Purity: 99.77% Purity: 97.76% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg (RS)-Butyryltimolol (S)-Carvedilol Cat. No.: HY-102032A ((S)-BM 14190) Cat. No.: HY-B0006B (RS)-Butyryltimolol is the racemate of (S)-Carvedilol, the S-enantiomer of Carvedilol, is Butyryltimolol. Butyryltimolol, an effective a non-selective β/α-1 blocker. (S)-Carvedilol prodrug of Timolol, improves the corneal exerts protection against the vascular or cardiac penetration of Timolol. Butyryltimolol is a toxicity of Doxorubicin (DOX). β-adrenergic blocker. Purity: >98.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 1 mg, 5 mg (S)-Terazosin (S)-Timolol Maleate Cat. No.: HY-B0371D (L-714,465 Maleate; MK 950) Cat. No.: HY-17380 (S)-Terazosin is an active S-enantiomer of (S)-Timolol Maleate (L-714,465 Maleate) is a Terazosin. (S)-Terazosin is a potent and non-cardioselective hydrophilic β-adrenoceptor high-affinity α-adrenoceptor antagonist with Ki blocker. (S)-Timolol Maleate is widely used as values of 3.91 nM, 0.79 nM and 1.16 nM for α1a, standard medication for intraocular pressure α1b and α1d-adrenoceptor, respectively. (glaucoma) by preventing the production of aqueous humor. Purity: 99.77% Purity: 99.85% Clinical Data: No Development Reported Clinical Data: Launched Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 100 mg, 200 mg 2 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] (±)-Befunolol (±)-Bisoprolol hemifumarate Cat. No.: HY-101752 (Bisoprolol hemifumarate salt) Cat. No.: HY-B0076 (±)-Befunolol is a β-adrenoceptor blocking agent. (±)-Bisoprolol (hemifumarate) is a selective type β1 adrenergic receptor blocker. Target: Adrenergic Receptor Approved: July 31, 1992 Bisoprolol, on beta 1-adrenoceptor peptide induced autoimmune myocardial damage. Purity: >98% Purity: 99.65% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 50 mg, 100 mg, 200 mg, 500 mg 2',5'-Dideoxyadenosine 4-Hydroxypropranolol D7 hydrochloride Cat. No.: HY-135878 ((±)-4-hydroxy Propranolol D7 hydrochloride) Cat. No.: HY-100634S 2',5'-Dideoxyadenosine is a potent and 4-Hydroxypropranolol D7 hydrochloride non-competitive adenylyl cyclase inhibitor via ((±)-4-hydroxy Propranolol D7 hydrochloride) is a binding the P-site with an IC50 of 3 µM . deuterium labeled 4-Hydroxypropranolol 2',5'-Dideoxyadenosine is a nucleoside analog and hydrochloride. exerts a potent antiadrenergic action in heart. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg, 100 mg, 250 mg Size: 1 mg, 5 mg 4-Hydroxypropranolol hydrochloride 5-HT2 antagonist 1 ((±)-4-hydroxy Propranolol hydrochloride) Cat. No.: HY-100634 Cat. No.: HY-U00365 4-Hydroxypropranolol hydrochlorid is an active 5-HT2 antagonist 1 is a potent antagonist of metabolite of Propranolol. 4-Hydroxypropranolol 5-HT2 receptor, with weak α1 adrenoceptor hydrochlorid is of comparable potency to blocking activity. Propranolol. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg Aaptamine Acebutolol D7 Cat. No.: HY-N4225 Cat. No.: HY-17497S Aaptamine, a spongean alkaloid isolated from a sea Acebutolol D7 is a deuterium labeled Acebutolol. sponge Aaptos aaptos, is a competitive antagonist Acebutolol is a selective β1 adrenergic receptor of α-adrenoceptor and activates the p21 promoter antagonist used in the treatment of hypertension, in a p53-independent manner. angina pectoris and cardiac arrhythmias. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg Acebutolol hydrochloride ACTH (1-14) Cat. No.: HY-17497A (Adrenocorticotropic Hormone Fragment 1-14) Cat. No.: HY-P1582 Acebutolol hydrochloride is a β1 adrenergic ACTH (1-14) is a fragment of adrenocorticotrophin, receptor (β1AR) antagonist. Acebutolol which regulates cortisol and androgen production. hydrochloride is used in the treatment of hypertension, angina pectoris and cardiac arrhythmias. Purity: 99.95% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 100 mg, 5 g, 10 g Size: 1 mg, 5 mg www.MedChemExpress.com 3 ACTH (1-14) (TFA) ADRA1D receptor agonist 1 (Adrenocorticotropic Hormone Fragment 1-14 TFA) Cat. No.: HY-P1582A Cat. No.: HY-135270 ACTH (1-14) (TFA) is a fragment of ADRA1D receptor agonist 1 (compound (R)-9S) is a adrenocorticotrophin, which regulates cortisol and potent, selective and orally active α1D androgen production. adrenoceptor antagonist, with a Ki of 1.6 nM. Purity: 98.55% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 1 mg, 5 mg AGN 192836 Ajmalicine Cat. No.: HY-100300 (Raubasine) Cat. No.: HY-N1919 AGN 192836 is a potent and selective α2 adrenergic Ajmalicine (Raubasine) is found in herbs of agonist with EC50s of 8.7, 41 and 6.6 nM for Catharanthus roseus, is an antihypertensive drug α2A, α2B and α2C receptor, respectively. used in the treatment of high blood pressure, decreases peripheral resistance and blood pressure. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg Alfuzosin Alfuzosin hydrochloride (SL 77499) Cat. No.: HY-B0192 (SL 77499-10) Cat. No.: HY-B0192A Alfuzosin is an α1 adrenergic receptor antagonist Alfuzosin hydrochloride is an α1 adrenergic used to treat benign prostatic hyperplasia (BPH). receptor antagonist used to treat benign prostatic hyperplasia (BPH). Purity: 99.81% Purity: 98.73% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 10 mg, 50 mg Size: 10 mM × 1 mL, 10 mg, 50 mg Amezinium methylsulfate Amibegron hydrochloride (Amezinium metilsulfate; Lu-1631) Cat. No.: HY-A0275 (SR 58611A) Cat. No.: HY-103207 Amezinium metilsulfate has multiple mechanisms, Amibegron hydrochloride is a selective including stimulation of alpha and beta-1 β3-adrenoceptor agonist, with an EC50 of 3.5 nM receptors and inhibition ofnoradrenaline and for β-adrenoceptor in rat colon; Amibegron tyramine uptake. hydrochloride has anxiolytic and antidepressant activity. Purity: 99.51% Purity: >99.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 100 mg, 500 mg, 1 g Size: 5 mg Amitraz Ancarolol (BTS-27419) Cat. No.: HY-B1111 Cat. No.: HY-100141 Amitraz is a non-systemic acaricide and Ancarolol is a beta-adrenergic blocking agent. insecticide, with alpha-adrenergic agonist activity, interaction with octopamine receptors of the central nervous system and inhibition of monoamine oxidases and prostaglandin synthesis. Purity: >98.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 100 mg Size: 1 mg, 5 mg 4 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] AR-08 Arbutamine Cat. No.: HY-U00371 Cat. No.: HY-16056 AR-​08 is an agonist of α2-adrenergic receptor, Arbutamine is a short-acting synthetic potent used for the treatment of attention deficit nonselective β-adrenoceptor agonist that hyperactivety disorder (ADHD).