(3H)-Propranolol binding sites in myocardial membranes: nonidentity with beta adrenergic receptors.

نویسندگان

  • D E Vatner
  • R J Lefkowitz
چکیده

[3F1] Propnamioolool 1)iti(ii5 roopidly tiIi(h nO’vensil)lV to sites in mii(’miih)m’aIiO’s l)l’o’l)mir(’d fronts ‘atiiite vo-’mitnietolar Iti\’oocardiumil. ‘j’\\ j oot’do’rs oof sito’s wero’ identified. Tho’ htighto’r-order sito’s have a vmtluo’ (o’luilillniuni coonstmitit ) oof 4.57 X 10 ii-tm and a bimudimog cm-opacity of 3.2 X 10-s miioole/ trig oof’ Jlrooto’imo. 1’or thoo’ loowo’r-oordo’r sito’s K = 4.32 X 102 it-0 amid 1)itiolillg capacity is 8.4 )( 10 miioolo’/nig oof proito’imo. Nimio’ adro’mio’rgi(’ titutagoomuist drugs wo’t’e to’sted f’oor theim’ ability too blO(’k [31Ijpt’oopnmtmioolool I)itidilug amo(! bloick isoopnooto’ro’nool activmitioomi of ado’miylato’ cyclaso’ in dog hiettm’t moienil)raiuo’s. \oo o’lear o’o)rro’latioomi l)o’two’emo tho’ tivoo f’utuo’tionis ivtis f’oound. damid 1I nooprtitio olool o’olmiip(’tO’(l -it Ii equmil o’ffo’ctiveno’ss for t ho’ pm’oopm’amioolool bimidimug sites, but Ipnopranoolooi \\.tis )0 timito’s nioro’ Pooto’mit thotiii tlO(’ 0/ isolni(’r in bloocking o’yclmiso’ mtctivatioii. ‘The bo’tmi mtdno’moo’rgic blockimog agent di(’holoorooiso)pm’ooto’t’o’mtoil vas a vo’t’ ’ ivo’ak inhibitolr oof [3Hj_ propnmotooolool 1)ifldiflg. (1lilonproonimizimoo’ timid hmilopenidol inhihitod booth Prol)ramuolool bimidimog amid o’yclaso’ mi(’tivmitioomo. It is coomuo’ludod that the [3H]pm’opramiolool bimidimog sift’s stimdied loo’re art’ umtro’lttto’d too tin’ miiyooomiroiial beta tidro’moergio’ ro’o’o’ptors amid nimoy 1)o’ invoolvo’d iii niediating tho’ nioot’o’ go’moo’ral iuuo’muibramio’ or local ttmio’sthetic o’flo’(’ts of prooiom’amioolool . Beta adneno’rgic re(‘(‘9toor bimidimog sito’s bIresUtuumil)IY r(’I)reso’mut toooo smumuhl to frmictiono (If misvolcardial noemiihrt-imoe sito’s o’aptilllo’ (If bimoolimig proprmimioolol too he t’evo’a1o’d by bntdimig studio’s of this typo’.

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عنوان ژورنال:
  • Molecular pharmacology

دوره 10 3  شماره 

صفحات  -

تاریخ انتشار 1974