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.

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

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.

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

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.

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.

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.

Lapaquistat acetate (TAK-475) is a squalene synthase inhibitor with potential anti-inflammatory activity. It mitigates statin-induced toxicity in human skeletal muscle cells and protects guinea pigs from simvastatin-induced myotoxicity, useful for research on hypercholesterolemia and HMG-CoA reductase deficiency.

Rupatadine (UR-12592, rupatadine) is a potent and orally available dual antagonist of PAF and histamine H1 receptors with Ki values of 0.55 μM and 0.1 μM, respectively, which provides relief of allergic symptoms and anti-inflammatory properties, and is used in allergic rhinitis and chronic urticaria.

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.

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.

(+)-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.

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.

Toladryl is a derivative of Diphenhydramine that can cross the blood-brain barrier and exhibits oral activity, with antihistamine and anticholinergic properties. Its anticholinergic effects are approximately a tenth of those seen with Diphenhydramine, yet it offers 2-4 times the protection against lethal doses of histamine in guinea pigs. The side effects of Toladryl are fewer and milder compared to Diphenhydramine; however, at higher doses, it may cause symptoms such as insomnia, agitation, and disorientation related to the central nervous system. Toladryl is utilized in the research of allergic diseases.

DNBS, also known as 2,4-Dinitrobenzenesulfonic Acid (sodium salt), is a hapten. At concentrations of 25, 50, or 100 ppm, it can induce the proliferation of primary lymphocytes and epithelial cells derived from guinea pigs that are sensitive to 2,4-dinitrochlorobenzene (2,4-DNCB).

SR2640 is a potent and highly selective LTD4 LTE4 antagonist, specifically inhibiting LTD4-induced contractions in guinea pig ileum and tracheal smooth muscle in a concentration-dependent manner, without affecting histamine-induced contractions. It blocks the binding of 0.4 nM [3H]LTD4 to guinea pig lung membrane receptors with an IC50 of 23 nM. SR2640 also causes a parallel rightward shift in the dose-response curve for LTD4-induced bronchoconstriction in guinea pigs when administered intravenously, with the degree of shift correlating positively with its dosage. SR2640 is applicable for asthma research.

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

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

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

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

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

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.