contractions

Carboprost (15(S)-15-Methyl Prostaglandin F2α) is a synthetic analogue of PGF2α with oxytocic properties, commonly used to restore uterine tone.

Ethyl cinnamate has antifungal, and vasorelaxant effects. Ethyl cinnamate can lead to the damage of cell membrane system and metabolic disorder through inducing lipid peroxidation via initiating ROS overproduction. Ethyl cinnamate can inhibit the tonic contractions induced by high K+ and phenylephrine (PE) in a concentration-dependent manner, with respective IC50 values of 0.30 mM and 0.38 mM.

AS-35 is an orally effective, potent, and selective antagonist of leukotrienes, antagonizing LTC4-, LTD4-, and LTE4-induced ileum contractions with IC50 values of 8 nM, 4 nM, and 3 nM, respectively. It exhibits antiallergic activities.

SSR126768A is a novel and selective, orally active and potent oxytocin (OT) receptor antagonist with inhibitory effects on uterine contractions for the prevention of preterm labor.

Oxodipine, a dihydropyridine-type calcium antagonist, inhibited KCl-induced aortic contraction in rabbits and reduced cardiac force in less potent rat ventricular test-paper contractions. In rat cultured neonatal ventricular myocytes, Oxodipine reduced L-type Ca currents (I) with an IC of 0.24 μM, and against T-type Ca currents (I) with an IC of 0.41 μM. Oxodipine causes constipation in mice and gingival hyperplasia in dogs.

YM-58790 free base is a potent mAChR antagonist that inhibits M1 mAChR, M2 mAChR, and M3 mAChR with Ki values of 28 nM, 260 nM, and 15 nM, respectively. It inhibits reflex rhythmic bladder contractions in rats by inhibiting bladder pressurization.

Casanthranol, a concentrated mixture of anthranol glycosides from the dried bark of Rhamnus p. (cascara sagrada), is a stimulant laxative used to alleviate constipation and other medical conditions by increasing muscle contractions in the intestinal wall to facilitate bowel movements.

Ritodrine hydrochloride (NSC 291565) binds to and activates beta-2 adrenergic receptors of myometrial cells in the uterus, which decreases the intensity and frequency of uterine contractions. Ritodrine hydrochloride (NSC 291565) is a phenethylamine derivative with tocolytic activity. Specifically, Ritodrine hydrochloride (NSC 291565) probably activates adenyl cyclase, thereby increasing production of cyclic adenosine monophosphate (cAMP), which in turn enhances the efflux of calcium from vascular smooth muscle cells. A lack of intracellular calcium prevents uterine myometrial contractions. In addition, this agent may directly inactivate myosin light chain kinase, a critical enzyme necessary for the initiation of muscle contractions.

Praziquantel (Droncit) increases the permeability of the tegument of susceptible worms, resulting in an influx and increase in intra-tegumental calcium leading to rapid contractions and paralysis of the worm's musculature through a subsequent increase in levels of calcium in the sarcoplasmic reticulum. Praziquantel is a pyrazinoisoquinoline derivative with anthelminthic property. In addition, vacuolization of the tegumental syncytium and blebbing results in tegument disintegration, leads to antigen exposure and elicit host defense responses to the worm.

Fesoterodine fumarate (Toviaz) is the fumarate salt form of fesoterodine, a competitive muscarinic receptor antagonist with muscle relaxant and urinary antispasmodic properties. Fesoterodine is rapidly hydrolyzed in vivo into its active metabolite 5-hydroxymethyl tolterodine, which binds and inhibits muscarinic receptors on the bladder detrusor muscle, thereby preventing bladder contractions or spasms caused by acetylcholine.

Desloratadine (Sch34117) is a long-acting piperidine derivate with selective H1 antihistaminergic and non-sedating properties. Desloratadine diminishes the typical histaminergic effects on H1-receptors in bronchial smooth muscle, capillaries and gastrointestinal smooth muscle, including vasodilation, bronchoconstriction, increased vascular permeability, pain, itching and spasmodic contractions of gastrointestinal smooth muscle. Desloratadine is used to provide symptomatic relieve of allergic symptoms.

1-Hydroxybaccatin I possesses significant antinociceptive activity against p- benzoquinone-induced abdominal contractions.

Cyclobuxine D, a steroidal alkaloid extracted from Buxus microphylla, exhibits significant bradycardia effects on rat hearts and inhibits acetylcholine and Ba++-induced longitudinal muscle contractions in isolated rabbit jejunum.

NS19504 is an activator of Ca2+-activated K+ channel with EC50 of 11.0 µM. NS19504 shows relaxing effect on bladder smooth muscle spontaneous phasic contractions[1].

Carboprost tromethamine, a synthetic 15-methyl analogue of prostaglandin F2α, effectively promotes uterine contractions and significantly reduces bleeding during and post-delivery.

Dexloxiglumide is an orally active and selective cholecystokinin type A (CCKA) receptor antagonist and the pharmacologically active enantiomer of Loxiglumide, effectively inhibiting smooth muscle contractions induced by cholecystokinin-octapeptide (CCK-8), while displaying moderate, polarized, concentration-dependent, and pH-dependent Caco-2 permeability and increasing uptake of the MRP1 substrate fluorescein. Dexloxiglumide supports the mechanistic studies of gastrointestinal disorders and tumor-related smooth muscle and transporter biology.

YM-49598 iodide is a tachykinin NK-1 receptor antagonist. It inhibits drug-induced bladder contractions in rats with an IC50 of 11 μg/kg.

DEC-TA-870 is the de-ethoxycarbonylated metabolite of TA-870. In rabbits, DEC-TA-870 exhibits a mild relaxing effect on contractions induced by PGF2 alpha. Additionally, in vitro, DEC-TA-870 shows a weak vasodilatory effect distinct from dopamine, whereas TA-870, once converted into free dopamine in vivo, demonstrates its vasodilatory properties.

ANO1-IN-4 (Compound 10bm) is a reversible inhibitor of the calcium-activated chloride channel transmembrane protein 16A (TMEM16A, also known as ANO1), with an IC50 of 0.030 µM. It demonstrates good metabolic stability in rat liver microsomes and can inhibit spontaneous contractions in isolated mouse ileum.

(-)-9-Hydroxycorynantheidine (9-O-Desmethyl mitragynine) is a demethylated analog of Mitragynine, functioning as a selective and partial agonist for the μ-opioid receptor (μ-opioid receptor). This compound inhibits electrically stimulated twitch contractions in the guinea pig ileum.

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.

Acetylcholine perchlorate is the perchlorate salt of acetylcholine. Acetylcholine, an endogenous neurotransmitter at cholinergic synapses, could amplify the action potential of the sarcolemma following by inducing muscle contractions.

RCD405 is a bronchodilator that exerts a relaxing effect by directly acting on human airway smooth muscle (hASM), with an EC50 value of 12 μM for histamine-induced contraction and 45.71 μM for carbachol-induced contraction. It inhibits cholinergic and histaminergic tension and reduces contractions induced by electrical field stimulation (EFS). RCD405 shows potential for research in asthma and chronic obstructive pulmonary disease (COPD).

Tiaramide is an anti-inflammatory agent that inhibits the release of PGE2. It also reduces the increase in intracellular free Ca2+ levels caused by PGE2 and bradykinin, and it suppresses contractions induced by bradykinin.