guinea-pigs

Etomoxir is a carnitine palmitoyltransferase 1a (CPT-1a) inhibitor that inhibits fatty acid oxidation by inhibiting CPT-1a and inhibits palmitate oxidation in humans, rats, and guinea pigs. Etomoxir has an inhibitory effect on adenine nucleotide translocase and can inhibit macrophage polarization by disrupting CoA homeostasis.

Dalcotidine (KU 1257) is a novel histamine H2 receptor antagonist with histamine H9 receptor antagonistic activity and antisecretory effects.The Ki value for binding to guinea pig cerebral cortex was 0.040 The KB value for antagonism of histamine-induced positive chronotropic responses in the right atrium of isolate guinea pigs was 0.041.Dalcotidine improves the quality of ulcer healing, and may contribute to a reduction in ulcer recurrence and relapse rates.

Nesosteine Lithium is a novel mucoregulatory that inhibits Herxheimer microconvulsions in guinea pigs and inhibits ovalbumin-induced histamine release from sensitized trachea.Nesosteine Lithium protects against ovalbumin-induced bronchospasm but is ineffective against histamine- and acetylcholine-induced bronchospasm. Nesosteine Lithium protected against ovalbumin-induced bronchospasm but not histamine- and acetylcholine-induced bronchospasm.

Moxipraquine is a novel 8-aminoquinolone compound with anti-infective activity against Trypanosoma cruzi. Moxipraquine effectively inhibited parasitemia but did not eradicate infections in mice or guinea pigs. Moxipraquine was effective against experimental infections of Leishmania major, Lactobacillus mexicanus, and Lactobacillus brasiliensis, but was Ineffective.

WAY127093B racemate is the racemic mixture of WAY127093B, a phosphodiesterase IV inhibitor with demonstrated oral activity in rats and guinea pigs.

Peptide M acetate is a synthetic amino acid (18 amino acids in length which correspond to the amino acid positions 303-322 of bovine S-antigen: DTNLASSTIIKEGIDKTV). Peptide M acetate is capable of inducing experimental autoimmune uveitis in monkeys and Hartley guinea pigs as well as Lewis rats.

Symetine（L 16726） is a small molecule compound with antiparasitic activity that can be used to study amoebic liver abscesses in guinea pigs.

Sulukast is a potent inhaled leukotriene antagonist, which was found to be effective in preventing both leukotriene_x0002_and antigen-induced bronchospasm in guinea-pigs.

Rupatadine (UR-12592) is a potent dual PAF H1 antagonist with Ki values of 0.55 μM in rabbit platelet membranes and 0.1 μM in guinea pig cerebellum membranes.

L-Albizziin (2-Methoxyidazoxan monohydrochloride) is a highly potent selective antagonist of the alpha 2r adrenergic receptor, with little or no antagonistic effect on imidazoline. It has a significantly higher affinity for the alpha 2D adrenergic receptor (pKd9.7) in guinea pigs than for the alpha 2A adrenergic receptor (pKd8.2) in rabbits.

Fenspiride hydrochloride (Decaspiride) , an oxazolidinone spiro compound, is a drug used in the therapy of certain respiratory diseases. It is approved for use in Russia for the therapy of chronic and acute inflammatory diseases of ENT organs and the respiratory tract (like sinusitis, tracheobronchitis, otitis, laryngitis, and rhinopharyngitis), and for maintenance therapy of asthma.

1. Crotonoside (Isoguanosine) has much more active than adenosine in reducing the blood pressure in rabbits and cats, in decreasing the tone of isolated intestinal strips of the rabbit, guinea pig and hamster and in stimulating the isolated uterus of guinea pigs and hamsters. 2. Crotonoside inhibits the growth of S-18 and Ehrlich solid tumor in mice at the optimal doses of 96 mg kg day x 12 and 48 mg kg day x 12, with 1-T C values of 65% and 6%, respectively.

Neotuberostemonine (NTS) is one of the main antitussive alkaloids in the root of Stemona tuberosa Lour, it has a significant protective effect on bleomycin (BLM)-induced pulmonary fibrosis through suppressing the recruitment and M2 polarization of macroph

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 Prostaglandin E1 is a prostaglandin E1 analogue that has bronchodilator activity and can inhibit histamine-induced bronchoconstriction and cause relaxation of tracheal strips in isolated guinea pigs.

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 is a potent antiviral agent that increases arterial oxygen saturation in mice infected with the lethal vaccinia virus (IHD strain) and reduces viral replication in guinea pigs, thereby improving outcomes in congenital guinea pig cytomegalovirus (GPCMV) infection [1] [2].

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.

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.

(+)-Cevimeline hydrochloride hemihydrate ((+)-SNI-2011), a potent muscarinic receptor agonist, shows promise as a therapeutic candidate for xerostomia in Sjogren's syndrome. It exhibits a broad pharmacological profile across various systems in animal models including mice, rats, guinea pigs, rabbits, and dogs. Metabolism studies using rat and dog liver microsomes reveal rapid absorption with peak plasma concentrations (Cmax) within one hour post-oral administration and a half-life (t1 2) between 0.4 to 1.1 hours. Bioavailability is 50% in rats and 30% in dogs. Metabolic analysis shows species-specific differences: rats produce S- and N-oxidized metabolites, while dogs produce only N-oxidized metabolites. Sex-based pharmacokinetic differences were noted in rats but not in dogs. In vitro studies indicate cytochrome P450 (CYP) and flavin-containing monooxygenase (FMO) involvement in the sulfoxidation and N-oxidation of SNI-2011, with CYP2D and CYP3A mainly responsible for sulfoxidation in rat liver microsomes.

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

Symetine dihydrochloride (L 16726 dihydrochloride) is the bis-hydrochloride form of Symetine. It exhibits antiprotozoal activity against Entamoeba histolytica and can ameliorate amoebic liver abscesses in guinea pigs.

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.

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.

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.

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

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.

Experimental allergic encephalitogenic peptide (human), an EAE peptide, induces encephalomyelitis in guinea pigs [1].

(R)-(+)-Deoxyarbutin, an isomer of deoxyarbutin, acts as a tyrosinase inhibitor. Effective at a concentration of 21 µM, it diminishes tyrosinase activity and has been demonstrated to lighten the skin in hairless guinea pigs with dark, medium, and light pigmentation when applied at a 1% concentration.

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

CHF-6366 is a dual-action chemical compound acting as a potent M3 muscarinic antagonist and β2-adrenergic receptors agonist, with respective pK i values of 10.4 and 11.4. Additionally, it exhibits weak calcium channel inhibitory properties (IC 50 ~50 μM) and demonstrates the ability to inhibit bronchoconstriction in guinea pigs, making it a viable candidate for chronic obstructive pulmonary disease (COPD) research.

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.

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

Apafant (WEB 2086) is a highly potent platelet activating factor (PAF) antagonist that blocks eosinophil activation and can be used to study experimental allergic conjunctivitis in guinea pigs.

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

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.

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

Tipelukast (KCA 757) is a novel, orally available leukotriene receptor antagonist with anti-inflammatory properties, capable of reducing fibrosis and down-regulating TIMP-1 and type 1 collagen. Tipelukast is utilized in asthma research.

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), a novel muscarinic receptor agonist, is being explored as a potential treatment for xerostomia in Sjogren's syndrome, exhibiting an IC50 value indicative of its affinity for mAChR. This compound's pharmacological effects on the gastrointestinal, urinary, and reproductive systems, alongside its impact on various tissues, were thoroughly examined in species including mice, rats, guinea pigs, rabbits, and dogs. The metabolic breakdown of (-)-SNI-2011 was studied in vitro using rat and dog liver microsomes to assess its biotransformation. Upon oral administration, peak plasma concentrations were reached within an hour in both rats and dogs, showcasing rapid absorption and a subsequent decrease in concentration with a half-life ranging from 0.4 to 1.1 hours. Bioavailability was noted at 50% in rats and 30% in dogs. Metabolic pathways highlighted significant species differences, with both S- and N-oxidized metabolites identified in rats, but only N-oxidized metabolites in dogs. Additionally, gender differences in pharmacokinetics were observed in rats but were absent in dogs. In vitro studies pinpointed the involvement of cytochrome P450 (CYP) and flavin-containing monooxygenase (FMO) in the metabolism of (-)-SNI-2011, specifically through sulfoxidation and N-oxidation processes, respectively. CYP2D and CYP3A were identified as the primary enzymes responsible for sulfoxidation in rat liver microsomes.

1. Crebanine iv 5mg kg can eonvert BaCl_2-induced arrhythmia into sinus rhythm in rats, and can significantly increase the tolerant dose of aconitine to produce ventrieular fibrillation(VF) and cardiac arrest (CA) in rata. 2. Crebanine can also decrease t

Ritolukast (Wy-48252), an orally active aerosol leukotriene (LTD 4 E 4) receptor antagonist, effectively inhibits bronchoconstriction induced by aerosol LTD 4 in guinea pigs, demonstrating an ID 50 of 0.5mg kg [1].