Nonpeptide antagonists for peptide receptors
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Nonpeptide antagonists for peptide receptors
| Angiotensin receptors
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| Receptor subtypes | AT1 | AT2 | ||
| Endogenous ligands | Ang II > Ang III | Ang II = Ang III | ||
| Selective antagonists | losartan (DuP753, MK954), DuP532, MK966 (L159282), irbesartan (SR47436, BMS186295), telmisartan (BIBR277), SKF108566, candesartan (TCV116, CV11974), valsartan (CGP48933), L158809, SC51316, SC51895, SC52458, ICID6888, ICID8731, A81282, A81988, GR117289, BMS180560, EXP3174, EXP3892, EXP3312, UP269-6, LR-B/081, UR7198, UR7280, E4177, CS866, DMP811 (L708404) | PD123177, PD123319 L161638 | ||
| Mixed AT1/AT2 antagonist | BIBS39, BIBS222, L163017, XR510 | |||
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| Bombesin receptors
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| Receptor subtypes | BB1 | BB2 | BB3 | |
| Endogenous ligands | NMB ≥ BB > GRP | GRP ≥ BB ≫ NMB | BB ≫ GRP = NMB | |
| Selective antagonists | PD165929 | KuwanonH | - | |
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| Bradykinin receptors
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| Receptor subtypes | B1 | B2 | ||
| Endogenous ligands | kallidin > BK | kallidin ≥ BK | ||
| Selective antagonists | - | WIN 64338 FR173657 | ||
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| Corticotropin-releasing factor receptors
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| Receptor subtypes | CRF1 | CRF2α | CRF2β | |
| Endogenous ligands | urocortin > CRF | Urocortin ≫ CRF | urocortin ≫ CRF | |
| Selective antagonist | CP154526 NB127914 antalarmin | - | - | |
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| Endothelin receptors
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| Receptor subtypes | ETA | ETB | ||
| Endogenous ligands | ET-1 = ET-2 > ET-3 | ET-1 = ET-2 = ET-3 | ||
| Selective antagonists | BMS182874, PD155080, PD156707, PD159110, PD159433, TBC11251, A127722, 97–139 | Ro468443 | ||
| Mixed ETA/ETB antagonists | bosentan (Ro470203), Ro462005, SB209670, SB209598, SB217242, L749329, L754142, L751281, PD154804, PD159020 | |||
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| Opioid receptors
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| Receptor subtypes | μ | δ | κ | |
| Endogenous ligands | β-end > dynA > met > leu | β-end = leu = met > dynA | dynA ≫ β-end > leu = met | |
| Selective antagonists | - | naltrindole BNTX NTB | nor-binaltorphimine (nor-BNI) | |
| Nonselective antagonists | naloxone, naltrexone* | |||
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| Vasopressin and oxytocin receptors
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| Receptor subtypes | V1A | V1B | V2 | OT |
| Endogenous ligands | VP > OT | VP > OT | VP>OT | OT ≥ VP |
| Selective antagonists | SR49059, OPC21268 | - | OPC31260 | L367773, L368899 L371257 |
| Mixed V1A/V2 antagonist | YM087 | |||
Abbreviations: Ang II, angiotensin II; Ang III, angiotensin III; β-end, β-endorphin; BB, bombesin; BK, bradykinin; CRF, corticotropin-releasing factor; dynA, dynorphin; ET-1, endothelin 1; ET-2, endothelin 2; ET-3, endothelin 3; GRP, gastrin-releasing peptide; kallidin, lysyl-bradykinin; leu, [Leu]enkephalin; met, [Met]enkephalin; NMB, neuromedin B; OT, oxytocin; VP, vasopressin.