“angiotensin receptors”的搜索结果
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angiotensin II and endothelin A receptor antagonist
Sparsentan (RE-021) is a highly potent dual angiotensin II and endothelin A receptor antagonist with Kis of 0.8 and 9.3 nM, respectively.
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GPR119 receptors agonist
PSN632408 is an optimized agonist of GPR119 receptors that shows similar potency to OEA at both recombinant mouse and human GPR119 receptors, exhibiting EC50 values of 5.6 and 7.9 uM, respectively.
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5-HT2A and 5-HT2C receptors antagonist
Deramciclane has a high affinity for 5-HT2A and 5-HT2C receptors; it acts as an antagonist at both receptor subtypes and has inverse agonist properties at the 5-HT2C receptors without direct stimulatory agonist.
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opioid receptors agonist
DPI-3290 (Org 41793) is a potent and specific opioid receptors agonist with Ki values of 0.18 nM, 0.46 nM, and 0.62 nM for δ-, μ-, and κ-opioid receptors, respectively.
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AChE /M1/M2/5HT4/I2 inhibitor
MHP 133 is a drug with multiple CNS targets, and inhibits acetylcholinesterase (AChE) with Ki of 69 μM; also active against muscarinic M1 and M2 receptors, serotonin 5HT4 receptors, and imidazole I2 receptors.
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group III mGluR receptors agonist
O-Phospho-L-serine is the immediate precursor to L-serine in the serine synthesis pathway, and an agonist at the group III mGluR receptors (mGluR4, mGluR6, mGluR7, and mGluR8); O-Phospho-L-serine also acts as a weak antagonist for mGluR1 and a potent antagonist for mGluR2.
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5-HT1A/5-HT1B receptors agonist
RU 24969 is a selective agonist at the 5-HT1A and 5-HT1B receptors.
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peripheral oxytocin receptors agonist
Carbetocin (Lonactene; Duratocin) is an obstetric drug used to control postpartum hemorrhage and bleeding after giving birth; an agonist at peripheral oxytocin receptors.
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5-HT2A receptor antagonist
Lumateperone Tosylate is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a SERT blocker (Ki = 61 nM).
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5-HT1B/1D receptors agonist
Donitriptan is a potent, high efficacy agonist at 5-HT1B/1D receptors with pKis of 9.4 and 9.3, respectively.
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sigma-1 receptors modulator
E1R is a novel positive allosteric modulator of sigma-1 receptors.
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S1P antagonist
VPC 23019, an aryl amide-containing Sphingosine 1-phosphate (S1P) analog, is a competitive antagonist at the S1P1 and S1P3 receptors (pKi= 7.86 and 5.93, respectively) and an agonist at the S1P4 and S1P5 receptors (pEC50= 6.58 and 7.07, respectively).
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alpha-1 adrenergic receptors / mAChRs inhibitor
Anisodamine is an inhibitor of alpha-1 adrenergic receptors and mAChRs isolated from Chinese solanacea plant.
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5-HT2 receptors inhibitor
Nefazodone HCl is an inhibitor of 5-HT2 receptors, SERT, NET, and hERG K+ channels used to treat mood disorders. It decreases immobility time in the forced swim test.
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D3 receptor and D2 receptor partial agonist
Cariprazine is a novel antipsychotic drug candidate that exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM).
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group II (mGlu2/3) receptor agonist
Eglumegad (LY354740) is a highly potent and selective group II (mGlu2/3) receptor agonist with IC50s of 5 and 24 nM on transfected human mGlu2 and mGlu3 receptors, respectively.
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A2B adenosine receptor antagonist
MRS 1754 is a selective antagonist radioligand for A2B adenosine receptor with very low affinity for A1 and A3 receptors of both humans and rats.
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adenosine A1 receptor antagonist
Derenofylline (SLV 320) is a potent, selective and orally active adenosine A1 receptor antagonist, with Ki values of 1 nM, 200 nM and 398 nM for human A1, A3 and A2A receptors respectively.
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5-HT2 receptor antagonist
Ritanserin (R 55667) is a highly potent, relatively selective, orally active, long acting antagonist of 5-HT2 receptor, with an IC50 of 0.9 nM, less active on Histamine H1, Dopamine D2, Adrenergic α1, Adrenergic α2 receptors.
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5-HT7 receptor antagonist
SB269970 hydrochloride (SB-269970A) is a hydrochloride salt form of SB-269970, which is a 5-HT7 receptor antagonist with the pKi of 8.3, exhibits >50-fold selectivity against other receptors.
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mGluRs M3 agonist
L-APB is a potent and specific agonist for the group III mGluRs, with EC50s of 0.13, 0.29, 1.0, 249 μM for mGlu4, mGlu8, mGlu6 and mGlu7 receptors, respectively.
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5-HT2C receptor antagonist
SB 242084 is a 5-HT2C receptor antagonist(pKi=9.0) that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2B receptors respectively.
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5-HT2C receptor antagonist
SB 242084 hydrochloride is a 5-HT2C receptor antagonist(pKi=9.0) that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2B receptors respectively.
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endothelin (ET) receptor antagonist
Tezosentan (RO 610612) is an endothelin (ET) receptor antagonist, with pA2s of 9.5, 7.7 for ETA and ETB receptors, respectively.
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oxytocin receptor ligand
Oxytocin (α-Hypophamine) is a mammalian neurohypophysial hormone; its actions are mediated by specific, high-affinity oxytocin receptors; ligand of oxytocin receptor.
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κ-opioid receptor antagonist
JDTic is a highly selective antagonist for the κ-opioid receptor; without affecting the μ- or δ-opioid receptors.
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A3 adenosine receptor agonist
AB-MECA is a high affinity A3 adenosine receptor agonist, has high affinity for recombinant A1 and A3 receptors.
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5-HT2C receptor agonist
CP-809101 is a potent and selective 5-HT2C receptor agonist with pEC50 of 9.96/7.19/6.81 for human 5-HT2C/5-HT2B/5-HT2A receptors respectively.
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Adenosine A2A receptor antagonist
ST3932 is a metabolite of ST1535, acts as an antagonist of adenosine A2A receptor, with Kis of 8 nM and 33 nM for A2A and A1 receptors, respectively.
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Dopamine receptor blocker
Dicarbine blocks dopamine receptors in various brain parts and prevents the depression of the conditioned defence reflexes caused by stimulation of the mesencephalic portion of the reticular formation. Dicarbine could be used to treat patients with schizophrenia and alcoholic psychosis in clinical.
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5-HT receptor antagonist
Pizotifen is a serotonin antagonist which acts mainly at the 5-HT1, 5-HT2A, and 5HT2C receptors with some antihistamine activity.
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α-1 adrenergic receptor blocker
Doxazosin is an α-1 adrenergic receptor blocker that inhibits the binding of norepinephrine, which is released from sympathetic nerve terminals, to the α-1 receptors on the membrane of vascular smooth muscle cells. Blockages of the alpha-1 adrenergic action on the vascular smooth muscles lead to a decrease in vascular resistance and antihypertensive activity.
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Dopamine receptor antagonist
Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5.
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A1 adenosine receptors 拮抗剂
Proxyphylline是茶碱的衍生物,由于其心血管特性而被用作支气管扩张剂。它与A2腺苷受体(对于血小板,Ki = 850μM)选择性拮抗A1腺苷受体(对于牛脑,Ki = 82 nM)。
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β-adrenergic receptors 拮抗剂
Acebutolol HCl是一种β-肾上腺素能受体拮抗剂,用于治疗高血压,心绞痛和心律不齐。
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mGlu4 receptors modulator
VU 0364770是mGlu4受体的正变构调节剂,在表达mGlu4的HEK 293细胞中EC50值为290 nM。
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β-adrenergic receptors 激动剂
Cimaterol是β的有效激动剂;肾上腺素能受体(人β的pEC50 = 8.13、8.78和6.62;1β,2β和3β)。
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β3-adrenergic receptors 激动剂
BRL 37344 Na Salt是具有脂解活性的β3-AR(β3-肾上腺素能受体)选择性激动剂。
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alpha1/beta adrenergic receptors 拮抗剂
Labetalol HCl是选择性α1-肾上腺素能受体和非选择性β-肾上腺素能受体的双重拮抗剂。
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- Reiko Watanabe, .et al. Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration, J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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adenosine A2B receptors 拮抗剂
CVT-6883是一种选择性的A2B腺苷拮抗剂,代表了一种治疗心肺疾病的新型潜在方法。
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mGlu4 receptors modulator
VU 0361737是mGluR-4的选择性正变构调节剂(人和大鼠受体的EC50值分别为240和110 nM)。
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5-HT Receptors/D2 dopamine receptor 拮抗剂
Olanzapine (LY170053)对5-HT2血清素和D2多巴胺受体拮抗剂具有高亲和力。
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5-HT Receptors 拮抗剂
Ondansetron HCl (GR 38032F)是5-羟色胺5-HT3受体拮抗剂,主要用作止吐药,通常在化疗后用于治疗恶心和呕吐。
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Opioid Receptors 激动剂
BRL 52537 hydrochloride是一种高度选择性和有效的κ阿片类激动剂(Ki = 0.24 nM)。比吗啡强25倍。
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