pig-2

Methyl eugenol (4-allylveratrole) 是一种苯丙类化合物，存在于植物叶子、果实、根茎中，当植物相应的部位因食草动物进食而受损时，就会释放。它可用于消灭雄性东方果蝇。

Rupatadine(UR-12592,卢帕他定)是一种有效和可口服的PAF和组胺H1受体的双重拮抗剂，Ki 值分别为 0.55 μM 和 0.1 μM，能够缓解过敏症状并抗炎，可用于过敏性鼻炎和慢性荨麻疹。

AR-A 2 is a selective 5-HT1B receptor antagonist, with a high affinity to guinea pig cortex 5HT1B 1D and recombinant guinea pig 5-HT1B receptors (Ki: 0.24 and 0.47 nM) and with 10-fold lower affinity to guinea pig 5-HT1D receptor (Ki: 5 nM).

Glycolic acid oxidase inhibitor 1（compound 2 in table 1）是一种乙醇酸氧化酶 (glycolate oxidase) 抑制剂,从而减少肾结石的形成风险。还能够抑制由过敏反应引起的慢反应物质（SRS-A）引起的豚鼠回肠收缩，对过敏性疾病，如哮喘，具有治疗潜力。

CGP37157 (7-Chloro-5-(2-chlorophenyl)-1,5-dihydro-4,1-benzothiazepine-2(3H)-one) 是一种 Na+ Ca2+ 交换抑制剂，抑制 Na+ 诱导的豚鼠心脏线粒体中 Ca2+ 的释放，IC50 为 0.8 μM。

PPADS tetrasodiuma 是一种有效的 P2X 受体拮抗剂，也是是豚鼠气道平滑肌 Na Ca²⁺ 交换逆模式的抑制剂，对谷氨酸 NMDA毒性有神经保护作用。PPADS tetrasodiuma 抑制 P2X1、P2X-2、P2X-3 和 P2X-5。

AGU654 (Compound 44) 是一种效力强的mPGES-1选择性抑制剂，对mPGES-1的IC50值为2.9 nM。通过抑制mPGES-1，AGU654 阻断COX-1 2将花生四烯酸转化为前列腺素E2 (PGE2) 的通路，从而有效缓解炎症、疼痛及发热。在活化的人单核细胞衍生巨噬细胞和人全血模型中，AGU654 能选择性抑制细菌外毒素诱导的PGE2生成，同时不影响其他前列腺素的产生。在豚鼠模型中，它显著减轻了发热、炎症和炎症性疼痛，展现出显著的抗炎、镇痛和退热功效。AGU654 有潜力成为研究炎症性疾病和疼痛的新方法。

Phaclofen (3-Amino-2-(4-chlorophenyl)propanephosphonic acid) 是一种选择性 GABAB receptor 拮抗剂，可部分拮抗（-）-巴氯芬的镇静作用，可逆地拮抗巴氯芬或GABA对豚鼠回肠和远端结肠胆碱能抽搐反应的抑制，可用于研究神进系统疾病。

Piclamilast (RP 73401) 是一种有效的磷酸二酯酶 4(PDE4)的抑制剂，对猪主动脉和可溶性嗜酸性粒细胞中的 IC50值分别为 16 nM 和 2 nM。

AK-2-38 is a nifedipine analogue with potent smooth muscle calcium antagonist action and partial agonist effects on isolated guinea pig left atrium.

Delequamine HCl is a potent and selective alpha 2-adrenoceptor antagonist. Delequamine HCl has a pKi of 9.45 for alpha 2-adrenoceptors in the rat cortex (pA2 in the guinea-pig ileum of 9.72).

GS 283 is a Ca(2+) antagonist. GS 283 is also a weak histamine and muscarinic receptor blocker in rat and guinea pig tracheal smooth muscles.

GSK172981 is a non-peptide tachykinin NK3 receptor antagonist with a high affinity for the recombinant human (PK (I) value 7.7) and native guinea pig (PK (I) value 7.8) tachykinin NK3 receptor. In vitro, the functional evaluation showed that GSK172981 was

GSK256471 is a potent selective NK(3) antagonist that shows a high affinity for recombinant human (PK (I) value 8.9) and native guinea pig (PK (I) value 8.4) tachykinin NK(3) receptors. In vitro functional assessment showed that GSK256471 reduced the E(Ma

14S(15R)-EET is an oxylipin and a cytochrome P450 metabolite of arachidonic acid .114S(15R)-EET binds to isolated guinea pig monocytes with a Kivalue of 612.5 nM in a competitive binding assay using [3H]14(15)-EET.2It induces dilation of precontracted isolated canine epicardial arterioles (EC50= 4 pM) and denuded porcine subepicardial arterioles (EC50= 3 pM).3Unlike 14R(15S)-EET, 14S(15R)-EET does not inhibit COX in enzyme assays or isolated platelets.4 1.Daikh, B.E., Lasker, J.M., Raucy, J.L., et al.Regio- and stereoselective epoxidation of arachidonic acid by human cytochromes P450 2C8 and 2C91J. Pharmacol. Exp. Ther.271(3)1427-1433(1994) 2.Wong, P.Y.-K., Lai, P.-S., and Falck, J.R.Mechanism and signal transduction of 14 (R), 15 (S)-epoxyeicosatrienoic acid (14,15-EET) binding in guinea pig monocytesProstaglandins Other Lipid Mediat.62(4)321-333(2000) 3.Zhang, Y., Oltman, C.L., Lu, T., et al.EET homologs potently dilate coronary microvessels and activate BKCa channelsAm. J. Physiol. Heart Circ. Physiol.280(6)H2430-H2440(2001) 4.Fitzpatrick, F.A., Ennis, M.D., Baze, M.E., et al.Inhibition of cyclooxygenase activity and platelet aggregation by epoxyeicosatrienoic acidsJ. Biol. Chem.261(2)15334-15338(1986)

Arecaidine propargyl ester is an agonist of M2muscarinic acetylcholine receptors (mAChRs).1It selectively binds to M2over M1, M3, M4, and M5mAChRs in CHO cells expressing the human receptors (Kis = 0.0871, 1.23, 0.851, 0.977, and 0.933 μM, respectively). Arecaidine propargyl ester induces contractions in isolated guinea pig atrium (pD2= 8.67). It induces apoptosis and the production of reactive oxygen species (ROS) in U87 and U251 glioblastoma cells when used at a concentration of 100 μM.2Arecaidine propargyl ester decreases mean arterial blood pressure in normotensive cats (ED25= 1.9 nmol kg).3It is toxic to house flies (Musca) when administered at a dose of 75 μg fly.4 1.Scapecchi, S., Matucci, R., Bellucci, C., et al.Highly chiral muscarinic ligands: the discovery of (2S,2’R,3’S,5’R)-1-methyl-2-(2-methyl-1,3-oxathiolan-5-yl)pyrrolidine 3-sulfoxide methyl iodide, a potent, functionally selective, M2 partial agonistJ. Med. Chem.49(6)1925-1931(2006) 2.Di Bari, M., Tombolillo, B., Conte, C., et al.Cytotoxic and genotoxic effects mediated by M2 muscarinic receptor activation in human glioblastoma cellsNeurochem. Int.90261-270(2015) 3.Porsius, A.J., and Van Zwieten, P.A.Central action of some cholinergic drugs (arecaidine esters) and nicotine on blood pressure and heart rate of catsProg. Brain Res.47131-135(1977) 4.Honda, H., Tomizawa, M., and Casida, J.E.Insect muscarinic acetylcholine receptor: Pharmacological and toxicological profiles of antagonists and agonistsJ. Agric. Food Chem.55(6)2276-2281(2007)

Pyrindolol is a bacterial metabolite that has been found inS. alboverticillatus.1It inhibits neutral β-galactosidase by 50% under acidic, but not neutral, conditions when used at a concentration of 2 μg ml. It is selective for β-galactosidase isolated from bovine liver over β-galactosidases isolated from human, bovine, pig, and rat tissues and sialidases isolated fromC. perfringens,Streptomyces, and the H3N2 strain of influenza virus (IC50s = >250 μg ml for all).1,2 1.Aoyagi, T., Kumagai, M., Hazato, T., et al.Pyridindolol, a new β-galactosidase inhibitor produced by actinomycetesJ. Antibiot. (Tokyo)28(7)555-557(1975) 2.Kumagai, M., Aoyagi, T., and Umezawa, H.Inhibitory activity of pyridindolol on β-galactosidaseJ. Antibiot. (Tokyo)29(7)696-703(1976)

14-Anhydrodigitoxigenin is a cardenolide and a derivative of digitoxin.1 It reduces the activity of guinea pig heart Na+ K+-ATPase by 15% when used at a concentration of 10 μM.2

Galanin is a neuropeptide with diverse biological activities. [1][2][3][4][5] It binds to rat galanin (GAL) receptor subtypes GAL1-3 (IC50s = 0.339, 1.35, and 3.31 nM, respectively) and human GAL1-3 (IC50s = 0.288, 1.62, and 12.3 nM, respectively). [1] Galanin binds to and inhibits contraction of guinea pig gastric smooth muscle cells induced by carbachol . [2] In vivo, Galanin (6 nmol, i.c.v.) increases feeding behavior in rats and increases latency to hindpaw withdrawal in response to heat and mechanical stimulation in a rat model of carrageenin-induced inflammation when administered at a dose of 2 nmol injected into the nucleus accumbens.[3][4] Galanin (5 μg, i.c.v.) also inhibits acetylcholine release induced by scopolamine in the ventral hippocampus of freely moving rats. [5]

Methoctramine is a selective antagonist of M2 muscarinic acetylcholine receptors (IC50 = 6.1 nM in CHO-K1 cell membranes).[1] It is selective for M2 over M1, M3, M4, and M5 receptors (IC50s = 92, 770, 260, and 217 nM, respectively). In vitro, methoctramine inhibits acetylcholine-induced reductions in isolated guinea pig tracheal tube contractions when used at a concentration of 1 μM.[2] In vivo, methoctramine inhibits bradycardia and bronchoconstriction induced by acetylcholinein guinea pigs with ED50 values of 38 and 81 nmol kg, respectively. In a rat model of spinal cord injury, methoctramine suppresses bladder overactivity induced by the non-selective muscarinic acetylcholine receptor agonist oxotremorine M.[3]

Betamethasone 21-phosphate is a synthetic glucocorticoid.1It prevents increases in macrophage and eosinophil numbers in bronchoalveolar lavage fluid (BALF) and decreases in blood leukocyte numbers in a guinea pig model of parainfluenza-3 viral infection when administered at a dose of 8 mg/kg but does not prevent airway hyperresponsiveness after infection.2Betamethasone 21-phosphate inhibits cell infiltration into the aqueous humor in a rat model of endotoxin-induced uveitis when administered topically or subcutaneously at doses of 0.01-1% or 1 mg/kg, respectively.3It increases maximal lung pressure volume curves in fetal sheep when administered to pregnant ewes at 0.75 gestation at doses of 80 and 170 μg/kg.1Betamethasone 21-phosphate increases body weight, impairs learning and memory, increases anxiolytic behavior, and reduces hippocampal neurogenesis in CD-1 mice but reduces body weight and increases neurogenesis with no effect on anxiety in high-anxiety DBA/2 mice when administered at a dose of approximately 25 mg/kg per day in the drinking water for seven weeks.4Formulations containing betamethasone 12-phosphate and betamethasone acetate have been used in the treatment of severe allergic conditions and a variety of immune-related conditions. 1.Loehle, M., Schwab, M., Kadner, S., et al.Dose-response effects of betamethasone on maturation of the fetal sheep lungAm. J. Obstet. Gynecol.202(2)186.e181-186.e187(2010) 2.Leusink-Muis, A., Ten Broeke, R., Folkerts, G., et al.Betamethasone prevents virus-induced airway inflammation but not airway hyperresponsiveness in guinea pigsClin. Exp. Allergy29(Suppl. 2)82-85(1999) 3.Tsuji, F., Sawa, K., Kato, M., et al.The effects of betamethasone derivatives on endotoxin-induced uveitis in ratExp. Eye Res.64(1)31-36(1997) 4.Aiello, R., Crupi, R., Leo, A., et al.Long-term betamethasone 21-phosphate disodium treatment has distinct effects in CD1 and DBA/2 mice on animal behavior accompanied by opposite effects on neurogenesisBehav. Brain Res.278155-166(2015)

PB28 is a cyclohexylpiperazine derivative that functions as a potent and highly selective agonist of the sigma 2 (σ2) receptor, exhibiting a Ki (binding affinity) of 0.68 nM. At the same time, PB28 acts as an antagonist of the sigma 1 (σ1) receptor, with a Ki of 0.38 nM. PB28 demonstrates a lower affinity for other receptors. It effectively inhibits electrically evoked twitch in both the guinea pig bladder (EC50 value of 2.62 μM) and ileum (EC50 value of 3.96 μM). Moreover, PB28 exhibits the ability to modulate protein-protein interaction between SARS-CoV-2 and human cells. Additionally, PB28 triggers caspase-independent apoptosis and possesses significant antitumor activity.

Protostemonine 是一种主要从 Stemona sesslifolia 根中分离得到的生物碱，对哮喘及革兰氏阴性菌所致急性肺损伤有抗炎作用。

Praeruptorin E 是白花前胡中的一种主要成分，是钙拮抗剂，pD2′值为 5.2。