Bradykinin receptors

364 an human 7TM 366 aa rat (IJZSOZS) 7TM

(8.5-9.6)

ligands: bradykinin

(BK), BK,_,, kallidin (Lys-BK), T-kinin (Ile-Ser-BK), [Hyp”]bradykinin,

‘ides-Arg]BK; the presence of 8, receptors is most easity indicated by the activity of BK,,

Endogenous

are antagonists

[Hyp4]kallidin

Other receptors~inding sites: The existence of B, receptors in guinea-pig airways has been proposed. Certain [DPhe7J-subst~tuted analugues of bradykinin at B, receptors but are claimed to be inactive at B, receptors. The variation in pA, values of antagonists at 8, receptors may reflect the existence of receptor subtypes or species homologues.

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Structural information

IPJ DG b2

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Predominant effecters

[“H]DArg[Proz,HypJ,Thii,DTic’,Ticfi]BK [1251]-fTyr#]BK [W]BK

Gene

PHlBKj-s

Radioligands

~Hyp~,Tyr(M~)~]BK

Sarjt~PheRJBK,, HOE140 (7.5-10.5) uArg[Hyp”,ThiSs4uPhe7JBK (6.0-7.5) oArg[Hyp”,This,HypE(Ir9rrs-propyl)70icH]BK DAr~[~yp~,DPhe’,Leu~]BK (6.8-7.9)

~Phe”,~(~H~-NH)Ar~~]BK

B&.8*

Selective agonists

[LeuH]BKI_8(6.7-7.3) [des-Arg’“]HOEl40

knllidin 2 BK 2:’ BK,..,

BK,_, = kallidin > BK

l?otency order

Selective antagonists

EK2

F2

SKI

Bl

Previous names

Nomenclature