Adrenoceptors

A. L?nl. (3995) FEBS Lrftus

363, 2.46-266

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Plmrrmm~. RIT. 47.267-270

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Chemical names . AHllllOA: I-(biphenyl-2-yloxy) -!-imino-&piperidin-1-yl-hutan-2-<)1 . ARC239: 2-(2,-k-IO-methoxyphenyl]-piperazin)-l-y1 . BHT920: h-aLlyl-2-amino-5,6,7,8-tetrahydro-1VI-thiazolo-[~,~-d]-~~epine . BMY7378: 8-i2-[-(2-methoxyphenyl)-l-piperazinyl]ethy~]-S-aza~piro[1,E;ldecae-7.9-dione dihydrochlorlde . BRL37344: sr~dium-l-(2-[2-hydr~~y-(3-chlorophenyl}e~h~lamin~]~r~~p~l)phen~~~,~cctate CGP12177: ~-)~-(3-tert-bu~lamino-2-hydroxypropo~y)-benzim~da~ol-~-one CGP207lZA: 2-h~~drox~-5-(2-[[2-hydroxy-3-(~-[l-methyl-~~fluoromethyl-2-~midazolyl]phenr~xy)~ro~~l~amino~eth~~~~)~enz~m~~~e CL316243 &sod&m (R,R)-5-(2-([2-(3-chlorophenyl)-2-hydroxyeth~~]-~m~n~~~pro~~~)-l,3-benzodioxole-2,2-dicarbo~~-late HEAT: 2-P--t-h!rdroxy-3-iodophenylethylaminomethy1tehalone iCIlI8551: cr~thro-~~-1-(7-m~thyIindan4-yloxy)-3-isopropyl-aminobutanc-2-nl 1 vfD3213: (-)-(r~)-l-(3-ydroxy~ropyI]-5-(2-(2-(2-(2,2,2-~ifluor~thytho~~)pheno~~l~-ethylamino]prc~pyl]indoline-7 lrbovamlde a RS17053: .V-[2-(2-cyclo~ropylmethoxyphenoxy)ethyl]-~-chloro-~~,o-dimeth~i-~fl-indolc-3-ethanamide . RX821002: 7-(2-methoxy-l,-l-benzodioxan-2-yl)-2-imidazoline . SNAP5089: 2,h-dimcthl~~~-(Cnitrophenyl)-1,4-dihydropyridine-3,S-dirarbox~lic acid-N-[3-(-L,4-diphenylpiperidin-l-vl)~rop~ l]amidc methyl ester . ‘Vi)fcdrbnxamido~-(3-nitrophen~l SNAP5272: 5-carboxamide-2,6-diethyl-l,~-dihydro-3-~~-(3-[~-h~droa~-l-~hen)-lpipcridin-yl]p~ . UK14304: 5-bromo-6-[2-imidazolin-Z-ylamino]quinoxaline

Reviews l Bylund, D. 8. I+a/. (1994) Intemational Union of Pharmacology Nomenclature of Adrenoceptors PJ7nr~7nd. Jim 46, 12 l-l 3 l Emorinc, L. c-tnl. (1994) The human P,-adrenoceptor: the search for a phvsiological function Trcrltfs P~mrw~al. Sri. 15. ;-i l Giacobino, J-P. (1995) P,-adrenoceptor: An update Eur. 1. Edocrimd. 132, 3i7-38.5 l flieble, J. P. (1Y95) International Union of Pharmacology. X. Recommendation for nomenclature of rqadrenoceptors: Ctrncenws * Kobill.a, 8. K. (1992) Adrenergic receptors as models for G protein-coupLed receptors AII~I~I.RIT. Nr~uo_wi. 15,87-11-l

Reference: 1. Hirasawa,

Other receptors/binding sites: Some tissues possess a,-adrenoceptors that have relatively low affinib (less than 1 n\l) for prazosin and the!, may represent additional subtypes. Binding sites for imidazolines have been identified but their function is not known; catecholamines ha\-e a low affinity for these sites. There is evidence for species homologues of P,-adrenoceptors (see review by Emorine ~1al.)

Comment: Examples of agonists selective for the a,-adrenoceptor class relative to the a,-adrenoceptor class are phenylephrine, methoxamme and cirazoline; antagonists selective for a,-adrenoceptors relative to a,-adrenoceptors are prkosin (M-10.5) and corynanthine (6.5-7.5); radioligands are [“Hlprazosin (0.1 IIM) and [‘ZI]HEAT (0.1 nM; also known as BE2254). Examples of agonists selective for the az-adrenoceptor class relative to the a,-adrenoceptor class are LX14304 and BHT920; antagonists selective for or,-adrenoceptors relative to a,-adrenoceptors are rauwolscine (9.0) and yohimbine (9.0); radjoligands are [3H]rauurolscine (1 IIM), [“Hlyohimbine (1 nM), [“H]UK14304 and [“H]RX821002 (0.5 nn_I).