Adrenoceptors in GtoPdb v.2023.1

The nomenclature of the Adrenoceptors has been agreed by NC-IUPHAR Subcommittee on [64, 194]. Adrenoceptors, α1 three α1-adrenoceptor subtypes α1A, α1B and α1D are activated endogenous agonists (-)-adrenaline (-)-noradrenaline. -(-)phenylephrine, methoxamine cirazoline prazosin doxazosin antagonists considered selective for α1- relative to α2-adrenoceptors. [3H]prazosin [125I]HEAT (BE2254) relatively radioligands. S(+)-niguldipine also high affinity L-type Ca2+ channels. Fluorescent derivatives (Bodipy FLprazosin- QAPB) used examine cellular localisation α1-adrenoceptors. α1-Adrenoceptor as nasal decongestants; treat symptoms benign prostatic hyperplasia (alfuzosin, doxazosin, terazosin, tamsulosin silodosin, with last two compounds being α1A-adrenoceptor claiming relax bladder neck tone less hypotension); a lesser extent hypertension (doxazosin, terazosin). β2-adrenoceptor antagonist carvedilol is congestive heart failure, although contribution blockade therapeutic effect unclear. Several anti-depressants anti-psychotic drugs contributing side effects such orthostatic hypotension. α2 α2-adrenoceptor α2A, α2B α2C lower potency brimonidine talipexole rauwolscine yohimbine α2- [3H]rauwolscine, [3H]brimonidine [3H]RX821002 There species variations in pharmacology α2A-adrenoceptor. Multiple mutations α2-adrenoceptors have described, some associated alterations function. Presynaptic regulate many functions nervous system. clonidine, guanabenz affect central baroreflex control (hypotension bradycardia), induce hypnotic analgesia, modulate seizure activity platelet aggregation. clonidine an anti-hypertensive (relatively little used) counteracts opioid withdrawal. dexmedetomidine (also xylazine) increasingly sedative analgesic human [33] veterinary medicine sympatholytic anxiolytic properties. mirtazapine anti-depressant. subtype appears be involved neurotransmission spinal cord regulating catecholamine release from adrenal chromaffin cells. Although subtype-selective developed, none clinically they remain experimental tools. β β-adrenoceptor β1, β2 β3 Isoprenaline β-adrenoceptors α2-adrenoceptors, while propranolol (pKi 8.2-9.2) cyanopindolol 10.0-11.0) β1- β2- β3-adrenoceptors. (-)-noradrenaline, xamoterol (-)-Ro 363 show selectivity β2-adrenoceptors. Pharmacological differences exist between mouse β3-adrenoceptors, 'rodent selective' BRL 37344 CL316243 low efficacy at β3-adrenoceptor whereas CGP 12177 (low potency) L 755507 activate β3-adrenoceptors [88]. β3-Adrenoceptors resistant propranolol, but can blocked concentrations bupranolol. SR59230A reasonably does not discriminate β- [332] L-748337 more selective. [125I]-cyanopindolol, [125I]-hydroxy benzylpindolol [3H]-alprenolol radioligands that label adrenoceptors labelled higher (nM) [125I]-cyanopindolol together antagonists. ligands BODIPY-TMR-CGP12177 track level [8]. Somewhat β1-adrenoceptor (denopamine, dobutamine) short term cardiogenic shock but, chronically, reduce survival. β1-Adrenoceptor-preferring cardiac arrhythmias (atenolol, bisoprolol, esmolol) failure (metoprolol, nebivolol) combination other treatments betaxolol, metoprolol [528]. Cardiac treated blocks β2-adrenoceptors, well Short (salbutamol, terbutaline) long (formoterol, salmeterol) acting β2-adrenoceptor-selective powerful bronchodilators respiratory disorders. Many first generation (propranolol) block both β2-adrenoceptors there no therapeutically. agonist mirabegron overactive syndrome. evidence suggest metastasis certain types cancer [197].