guinea-pigs

Etomoxir 是肉碱棕榈酰转移酶 1a （CPT-1a） 抑制剂，通过抑制 CPT-1a 来抑制脂肪酸氧化，且抑制人、大鼠和豚鼠中棕榈酸酯的氧化。Etomoxir 对腺嘌呤核苷酸转位酶有抑制作用，可通过破坏CoA稳态来抑制巨噬细胞极化。

Dalcotidine (KU 1257) 是一种新型组胺H2受体拮抗剂，具有组胺H9受体拮抗活性和抗分泌作用，与豚鼠大脑皮层结合的Ki 值为0.040 对分离性豚鼠右心房组胺诱导的正变时反应的拮抗作用的KB 值为0.041。Dalcotidine 提高了溃疡愈合的质量，可能有助于降低溃疡的复发率和复发率。

Nesosteine Lithium 是一种新型的粘液调节剂，对豚鼠 Herxheimer 微休克具有抑制作用且抑制卵清蛋白诱导的组胺在致敏动物气管中的释放。Nesosteine Lithium 能够保护致敏动物免受卵清蛋白诱导的支气管痉挛但对组胺和乙酰胆碱诱导的支气管痉挛无效。

Moxipraquine 是一种新型的8-氨基喹诺酮类化合物，对克氏锥虫具有抗感染活性。Moxipraquine 能有效抑制寄生虫血症，但不能根除小鼠或豚鼠的感染。Moxipraquine 对重度利什曼原虫、墨西哥乳杆菌和巴西乳杆菌的实验性感染有效，但对巴西乳杆菌无效。

WAY127093B racemate 是WAY127093 B 的外消旋体。WAY127093B 是一种磷酸二酯酶IV 抑制剂，在大鼠和豚鼠中具有口服活性。

L-Albizziin (2-Methoxyidazoxan monohydrochloride) 是高效的 alpha 2r 肾上腺素受体选择性拮抗剂，对 imidazoline 拮抗作用很小或没有。它对 (豚鼠) alpha 2D 肾上腺素受体 (pKd9.7) 的亲和力明显高于 (兔子) alpha 2A 肾上腺素受体 (pKd8.2)。

Fenspiride hydrochloride (Decaspiride) 是一种口服活性的非甾体抗炎剂，是 H1-组胺受体的拮抗剂，可用于呼吸系统疾病的研究。

Crotonoside (Isoguanosine) 是从中草药巴豆中分离出来的一种天然产物。 它抑制 FLT3 和 HDAC3 6，有治疗急性髓性白血病 (AML)的研究潜力。

Neotuberostemonine 是一种结核分枝杆菌根中主要的止咳生物碱，能够阻碍巨噬细胞的募集和活化，从而减轻博来霉素 (Bleomycin) 诱导的肺纤维化。

Apafant (WEB 2086) 是一种高效的血小板活化因子 (PAF) 拮抗剂，可阻断嗜酸性粒细胞活化，可用于研究豚鼠实验性过敏性结膜炎。

Crebanine 是来自于韦诺萨千金藤的一种生物碱，通过抑制 MAPKs 和 Akt 信号通路表现出抗炎活性，还具有抗心律失常的作用。它可诱导人类癌细胞的 G1阻滞和凋亡。

Symetine（L 16726） 是一种具有抗寄生虫活性的小分子化合物，可用于研究豚鼠阿米巴肝脓肿。

Tipelukast (KCA 757) 是一种新型可口服的白三烯受体 (leukotriene receptor) 拮抗剂，是具有抗炎活性，可减少纤维化，下调 TIMP-1、1 型胶原蛋白。Tipelukast 可用于研究哮喘疾病。

Peptide M acetate 是一种合成多肽 (长度为 18 个氨基酸，对应于牛 S 抗原的氨基酸位置303-322: DTNLASSTIIKEGIDKTV)，能够在猴子和 Hartley 豚鼠以及 Lewis 大鼠中诱导实验性自身免疫性葡萄膜炎。

Sulukast 是一种有效的吸入白三烯拮抗剂，在豚鼠中被发现可有效预防白三烯和抗原诱导的支气管痉挛。

Rupatadine (UR-12592) is a potent dual PAF H1 antagonist with Ki of 0.55 0.1 uM(rabbit platelet membranes guinea pig cerebellum membranes).IC50 value:Target: PAF H1 antagonistin vitro: Rupatadine competitively inhibited histamine-induced guinea pig ileum contraction (pA2 = 9.29 + - 0.06) without affecting contraction induced by ACh, serotonin or leukotriene D4 (LTD4). It also competitively inhibited PAF-induced platelet aggregation in washed rabbit platelets (WRP) (pA2 = 6.68 + - 0.08) and in human platelet-rich plasma (HPRP) (IC50 = 0.68 microM), while not affecting ADP- or arachidonic acid-induced platelet aggregation [1]. The IC50 for rupatadine in A23187, concanavalin A and anti-IgE induced histamine release was 0.7+ -0.4 microM, 3.2+ -0.7 microM and 1.5+ -0.4 microM, respectively whereas for loratadine the IC50 was 2.1+ -0.9 microM, 4.0+ -1.3 M and 1.7+ -0.5 microM. SR-27417A exhibited no inhibitory effect [2].in vivo: Rupatadine blocked histamine- and PAF-induced effects in vivo, such as hypotension in rats (ID50 = 1.4 and 0.44 mg kg i.v., respectively) and bronchoconstriction in guinea pigs (ID50 = 113 and 9.6 micrograms kg i.v.). Moreover, it potently inhibited PAF-induced mortality in mice (ID50 = 0.31 and 3.0 mg kg i.v. and p.o., respectively) and endotoxin-induced mortality in mice and rats (ID50 = 1.6 and 0.66 mg kg i.v.) [1]. rupatadine treatment improved the declined lung function and significantly decreased animal death. Moreover, rupatadine was able not only to attenuate silica-induced silicosis but also to produce a superior therapeutic efficacy compared to pirfenidone, histamine H1 antagonist loratadine, or PAF antagonist CV-3988 [3]. [1]. Merlos M, et al. Rupatadine, a new potent, orally active dual antagonist of histamine and platelet-activating factor (PAF). J Pharmacol Exp Ther. 1997 Jan;280(1):114-21. [2]. Queralt M, et al. In vitro inhibitory effect of rupatadine on histamine and TNF-alpha release from dispersed canine skin mast cells and the human mast cell line HMC-1. Inflamm Res. 2000 Jul;49(7):355-60. [3]. Lv XX, et al. Rupatadine protects against pulmonary fibrosis by attenuating PAF-mediated senescence in rodents. PLoS One. 2013 Jul 15;8(7):e68631.

Symetine dihydrochloride (L 16726 dihydrochloride) 是 Symetine 的二盐酸盐形态，具有针对 Entamoeba histolytica 的抗原虫效力，并可改善豚鼠阿米巴肝脓肿。

11-deoxy Prostaglandin E1 是前列腺素 E1类似物，具有支气管扩张活性，可抑制组胺诱导的支气管收缩，引起离体豚鼠的气管条松弛。

Mabuterol, (S)- is a D isoform of Mabuterol, which is a selective β2 adrenoreceptor agonist. Mabuterol has been found to decrease the blood pressure in rats and increase heart rate and contractile force in guinea pigs. Mabuterol inhibited the positive inotropic effect of isoprenaline but has no effect on alpha-adrenergic, acetylcholine and histamine receptors.

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]

11-deoxy PGF1α is a synthetic analog of PGF1α. In whole animal studies, a dose of 32 mg/kg inhibited gastric acid secretion by 35%. 11-deoxy PGF1α is also known to cause rat uterine contractions at a dose 0.3 times that of PGF1α. It also exhibits vasopressor and bronchoconstrictor activities at about half the potency of PGF2α in guinea pigs.

Cyclic HPMPC 是有效的抗病毒剂，可以增加感染致死性牛痘苗病毒 (IHD 株) 小鼠的动脉氧饱和度水平。用 Cyclic HPMPC 治疗可改善先天性豚鼠巨细胞病毒 (GPCMV) 感染的结果并减少豚鼠模型中的病毒复制。

(+)-Cevimeline hydrochloride hemihydrate ((+)-SNI-2011) 是一种有效的 mAChR 激动剂。

Lincydomine is a smooth muscle relaxant, beneficial to the treatment of unstable angina pectoris, but also can open the respiratory tract of humans and guinea pigs.

Luvangetin may have anti-inflammatory activity, it can inhibit NO and PGE2 production in LPS-stimulated BV2 cells. Luvangetin shows significant protection against pylorus-ligated and aspirin-induced gastric ulcers in rats and cold restraint stress-induced

Experimental allergic encephalitogenic peptide (human) 为EAE多肽类化合物，能够诱导豚鼠发生脑脊髓炎。

Mabuterol, (R)- is a D isoform of Mabuterol, which is a selective β2 adrenoreceptor agonist. Mabuterol has been found to decrease the blood pressure in rats and increase heart rate and contractile force in guinea pigs. Mabuterol inhibited the positive inotropic effect of isoprenaline but has no effect on alpha-adrenergic, acetylcholine and histamine receptors.

F-050 is a biochemical that has been shown to inhibit platelet aggregation induced by CaCl2, arachidonic acid, collagen, adenosine diphosphate (ADP) and thrombin in guinea pigs, rabbits and rats in vitro. F-050 may be useful in the treatment of thrombotic diseases.

Prostaglandin F2β (PGF2β) is the 9β-hydroxy stereoisomer of PGF2α. It is much less active than PGF2α in antifertility and bronchoconstrictor activities. PGF2β exhibits bronchodilating activity in guinea pigs and cats and antagonizes the bronchoconstrictor activity of PGF2α.

Btm 1042 is an antispasmodic drug. It has been found to depress twitch responses in the ileum of guinea pigs.

Eupatoriopicrin shows anti-trypanosomal activity and cytotoxicity against Trypanosoma brucei rhodesiense. Eupatoriopicrin-induced DNA damage may play a role in the observed cytotoxicity, it shows a weak sensitizing capacity in guinea pigs.

SUN-1334H free base 是一种口服有效的组胺 H1 受体抑制剂，IC50为 20.3 nM，Ki为 9.7 nM。它能够抑制由组胺引起的豚鼠离体回肠收缩，其IC50为 0.198 μM，并可抑制组胺导致的豚鼠支气管收缩、比格犬皮肤风疹及卵清蛋白引起的豚鼠鼻炎。

Des-4-fluorobenzyl Mosapride, the main metabolite of mosapride, acts as a gastroprokinetic agent improving upper gastrointestinal (GI) motility by stimulating the serotonin receptor 4 (5-HT4; EC50= 74.2 nM, in guinea pig ileal longitudinal muscle myenteric plexus). It has been shown to increase colonic motility in dogs, horses, and guinea pigs in vivo. Mosapride, including this metabolite, is utilized in human and veterinary medicine to mitigate post-surgical and Parkinson's-induced constipation.

CHF-6366是一种高效的M3毒蕈碱拮抗剂和β2肾上腺素能受体激动剂，具有pKi值分别为10.4和11.4。同时，CHF-6366作为一种弱钙离子通道抑制剂，其IC50约为50μM。该化合物能够抑制豚鼠的支气管收缩，适用于慢性阻塞性肺疾病研究。

(R)-(+)-Deoxyarbutin 是 deoxyarbutin 的一个异构体，同时也是一种酪氨酸酶抑制剂。在 21 µM 的浓度下，它能够抑制酪氨酸酶的活性。(R)-(+)-Deoxyarbutin (1%) 能够使无毛的深色、中等和浅色皮肤豚鼠的皮肤变亮。

AR-12456 is a Trapidil derivative that prevents serum hyperlipidemia in guinea pigs.

11-deoxy PGF1β is a synthetic analog of PGF1β. In contrast to PGF2α and PGF1α, 11-deoxy PGF1β exhibits vasodepressor and bronchodilator activities in guinea pigs at a dose of 500 μg kg.

Potent γ-secretase inhibitor (IC50 values are 1.2 and 6.2 nM in whole cell and cell-free assays, respectively). Reduces Aβ in brain, CSF and plasma in mice and guinea pigs. Lanz et al (2010) Pharmacodynamics and pharmacokinetics of the gamma-secretase inhibitor PF-3084014. J.Pharmacol.Exp.Ther. 334 269 PMID:20363853

Ambrein is a triterpene alcohol that is the chief constituent of ambergris, a secretion from the digestive system of the sperm whale, and has been suggested as the possible active component producing the supposed aphrodisiac effects of ambergris. It serves as the biological precursor for a number of aromatic derivatives such as ambroxan and is thought to possess fixative properties for other odorants. It has been shown to act as an analgesic and it has been proven to increase sexual behavior in rats, providing some support for its traditional aphrodisiac use. Ambrein has also been shown to decrease spontaneous contractions of smooth muscles in rats, guinea pigs, and rabbits. It is able to reduce these contractions by serving as an antagonist and interfering with the Ca2+ ions from outside of the cell.

Parogrelil is a phosphodiesterase (PDE3 PDE5A) inhibitor potentially for the treatment of intermittent. Parogrelil suppress the asthmatic response in guinea pigs, with both bronchodilating and anti-inflammatory effects. Parogrelil improves reduced walking

LY 302148 , a 5-HT1F receptor agonist, inhibits neurogenic dural inflammation in guinea pigs. It has potential for migraine therapeutics.

Ritolukast (Wy-48252) 是一种口服活性的气溶胶白三烯 (LTD4 E4) 受体拮抗剂，可用于抑制气溶胶 LTD4 引起的豚鼠支气管收缩，ID50 为 0.5 mg kg。

D-Mabuterol hydrochloride is a D isoform of Mabuterol, which is a selective β2 adrenoreceptor agonist. Mabuterol has been found to decrease the blood pressure in rats and increase heart rate and contractile force in guinea pigs. Mabuterol inhibited the positive inotropic effect of isoprenaline but has no effect on alpha-adrenergic, acetylcholine and histamine receptors.

(-)-Cevimeline hydrochloride hemihydrate ((-)-SNI-2011) 是一种新型mAChR 激动剂，是一种治疗干燥综合征口干症的候选治疗药物。