Proteina G/GPCR

GLP-1R agonist 12 (Compound 123) 是一种 GLP-1R 激动剂，能够用于研究糖尿病。

(R)-Casopitant ((R)-GW679769), an NK1-receptor antagonist, is used in chemotherapy-induced nausea research.

Indeloxazine HCl: Serotonin releaser, NE reuptake inhibitor, NMDA antagonist; antidepressant that boosts acetylcholine in rats.

<p>NBI-35965 is a CRF1 receptor antagonist.</p>

<p>S1P5-selective agonist; less so for S1P1/S1P3; useful for CNS disorders.</p>

CP 154,526 is a selective CRF1 receptor antagonist (Ki = 2.7 nM). CP 154,526 blocks CRF-induced activation of adenylate cyclase and the HPA axis.

PD 165929 is a selective antagonist of Bombesin BB1.

GSK2263167 is an agonist of S1P1 receptor.

TASP0376377 is a potent antagonist of CRTH2.

gonadotropin-releasing hormone (GnRH, LHRH) receptor antagonist,orally active

Frovatriptan, potent 5-HT 1B/D agonist, shows high cerebroselectivity and efficacy for migraine with aura.

<p>PSNCBAM-1 (PSNCBAM 1) is a CB1 receptor negative allosteric modulator (EC50 = 0.1 μM) with hypophagic effects in vivo.</p>

EX-1314 (BMS-604992) is a growth hormone secretagogue receptor (GHSR) agonist.

Pecavaptan is a vasopressin receptor antagonist.

Satigrel is a new antiplatelet agent. It also inhibits platelet accumulation in prosthetic arterial grafts.

17-Phenyl trinor Prostaglandin F2αdiethyl amide (17-phenyl trinor PGF2αdiethyl amide) is a Prostaglandin F2α(PGF2α) analog characterized by the substitution of the C-1 carboxyl group with an N-diethyl amide. Prostaglandin (PG) esters and N-ethyl amides have demonstrated ocular hypotensive properties, with N-ethyl amides introduced as alternative options for PG hypotensive prodrugs. Studies indicate that both bovine and human corneal tissues can convert N-ethyl amides of various PGs into their free acid forms at a rate of approximately 2.5 µg/g corneal tissue/hr. However, dialkyl amides like 17-phenyl trinor PGF2αdiethyl amide resist conversion by corneal amidase, showing no detectable transformation into free acids. This characteristic suggests their potential as valuable investigative tools for assessing the intrinsic intraocular hypotensive activities of PG amides.

TA-1887: Selective SGLT2 inhibitor, treats type 2 diabetes, lowers glucose in high-fat diet mice, boosts UGE, has good pharmacokinetics.

<p>TC-SP 14 (compound 14) is a potent, orally available S1P1 agonist with EC50 of 0.042 μM; minimal S1P3 binding (EC50 3.47 μM); reduces blood lymphocytes.</p>

<p>GSK-554418A, a novel azaindole CB(2) agonists, is used for the treatment of chronic pain. It is efficacious in the acute model and the chronic joint pain model.</p>

ONO-2050297 is the first potent dual CysLT1 and CysLT2 antagonist with IC50 values of 0.017 μM (CysLT1) and 0.00087 μM (CysLT2), respectively.