Bradycardia

Lerisetron is an antagonist of serotonin type 3 (5-HT3) receptor, with antiemetic activity.

YM-46303 is a selective and potent muscarinic receptor antagonist that exhibits high affinity for the M3 receptor.YM-46303 can be used to study bradycardia in medullary rats.

mTOR HDAC-IN-1 (Compound 50) is a dual inhibitor of mTOR and HDAC, with IC50 values of 0.49 nM and 0.91 nM, respectively, holding potential as an anti-cancer agent [1].

Bencycloquidium Bromide is a muscarinic M3 antagonist. Bencycloquidium bromide inhibits nasal hypersecretion in a rat model of allergic rhinitis. Bencycloquidium Bromide showed high affinity toward the M(3) receptor in Chinese hamster ovary (CHO) cells (M(1) pKi=7.86, M(2) pKi=7.21, M(3) pKi=8.21); pA(2)=8.85, 8.71 and 8.57 in methacholine-induced contraction of trachea, ileum and urinary bladder, 8.19 in methacholine-induced bradycardia of right atrium in vitro, respectively.This compound is unstable in powder form and other related salt forms are recommended.

Atropine (DL-Hyoscyamine) Sulfate is the sulfate salt of atropine, a naturally-occurring alkaloid isolated from the plant Atropa belladonna. Atropine functions as a sympathetic, competitive antagonist of muscarinic cholinergic receptors, thereby abolishing the effects of parasympathetic stimulation.

Isoprenaline (Norisodrine) is a non-selective and orally active β-adrenoceptor agonist.Isoproterenol is a potent peripheral vasodilator and bronchodilator.Isoproterenol can be used in the study of bradycardia and bronchial asthma for the treatment of heart block, bradycardia.

Atropine sulfate (Sulfatropinol) is a competitive antagonist for muscarinic acetylcholine receptor.

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.

Indisetron Dihydrochloride is a 5-HT(3) and 5-HT(4) receptor antagonist. Indisetron reduces 2-methyl-5-serotonin (HT)-induced bradycardia.

Lycorenine may produce a decrease in blood pressure as the result of alpha-adrenergic blockade in conjunction with the reduction of the spontaneous sympathetic nerve activity, and produce bradycardia by modifying vagal activity. The development of tachyph

CVT-2759 is A potential partial agonist for A(1)-ADORs, and it may be useful to slow atrioventricular node conduction to reduce ventricular rate without causing the atrioventricular block, bradycardia, atrial arrhythmias, or vasodilation.

Dalapon is a selective herbicide used to control perennial grasses. The major use of dalapon is on food crops including sugarcane and sugar beets. Its use is no longer authorized in France. The National Institute for Occupational Safety and Health in the

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]

Methoctramine tetrahydrochloride is a potent and cardioselective antagonist of the M2 muscarinic receptor, capable of inhibiting muscarine-induced bradycardia in vivo.

MDL-72567 is a dihydropyridine calcium antagonist that causes vasodilation and direct sinus bradycardia.

VCP-746 is a potent adenosine A2B receptor agonist that stimulates anti-fibrotic signalling. VCP746 reduces hypertrophy in a rat neonatal cardiac myocyte model. VCP746 is a hybrid molecule consisting of an adenosine moiety linked to an adenosine A1 receptor (A1AR) allosteric modulator moiety. At the A1AR, VCP746 mediated cardioprotection in the absence of haemodynamic side effects such as bradycardia.

Indisetron is a 5-HT(3) and 5-HT(4) receptor antagonist. Indisetron reduces 2-methyl-5-serotonin (HT)-induced bradycardia.

Melperone, a butyrophenone tranquillizer, caused bradycardia in vivo and in vitro.

(-)-Isoproterenol hydrochloride is used as a β-adrenergic receptor agonist in the treatment of bradycardia and as a bronchodilator.

Amiselimod (MT-1303) acts as a modulator for the sphingosine 1-phosphate receptor (S1P receptor). It converts to its active metabolite, (S)-amiselimod phosphate, through the action of sphingosine kinases (SPHKs), specifically targeting the S1P1 receptor. This results in improvement of autoimmune disease symptoms without inducing bradycardia.

HS024 is a highly potent melanocortin MC4 receptor antagonist (Ki values are 0.29, 18.6, 5.45 and 3.29 nM for cloned human MC4, MC1, MC3 and MC5 receptors respectively). Increases food intake, and blocks α-MSH- and MTII-induced hypotension and bradycardia in rats, following central administration in vivo.