A muscarinic receptor antagonist (Kis = 0.48

Biperiden (hydrochloride) – 5 mg

Brand:
Cayman
CAS:
1235-82-1
Storage:
-20
UN-No:
Non-Hazardous - /

Biperiden is a muscarinic acetylcholine receptor antagonist of (Kis = 0.48, 6.3, 3.9, 2.4, and 6.3 nM for M1-5 receptors, respectively, in CHO-K1 cells expressing cloned receptors).{22786} It inhibits binding of [3H]quinuclidinyl benzilate (QNB) to muscarinic receptors in tissue homogenates (IC50s = 79, 52, and 38 nM for rat heart, rat lung, and guinea pig lung, respectively) and in vivo (IC50s = 2.5, 1.1, and 1.2 mg/kg for mouse cerebral cortex, cerebellum, and heart, respectively).{39393,39394} Biperiden (1 μM) increases spontaneous and electrically-evoked dopamine (DA) and electrically-evoked acetylcholine (ACh) release from rabbit caudate nucleus slices preincubated with dopamine in vitro.{39395} It is also an uncompetitive NMDA receptor antagonist and inhibits NMDA-evoked ACh release at a concentration of 10 μM.{39396} Biperiden (0.01-1.0 mg/kg) reduces physostigmine-induced tremor in rats in a dose-dependent manner.{39397} Formulations containing biperiden have been used as an adjuvant treatment for Parkinson’s disease.  

 

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Description

A muscarinic receptor antagonist (Kis = 0.48, 6.3, 3.9, 2.4, and 6.3 nM for M1-5 receptors, respectively); inhibits binding of [3H]QNB to muscarinic receptors in tissue homogenates (IC50s = 79, 52, and 38 nM for rat heart, rat lung, and guinea pig lung, respectively) and in vivo (IC50s = 2.5, 1.1, and 1.2 mg/kg for mouse cerebral cortex, cerebellum, and heart, respectively); increases spontaneous and electrically-evoked DA and electrically-evoked ACh release from preincubated rabbit caudate nucleus slices in vitro when used at a concentration of 1 μM; an uncompetitive NMDA receptor antagonist and inhibits NMDA-evoked ACh release (10 μM); reduces physostigmine-induced tremor in rats in a dose-dependent manner (0.01-1.0 mg/kg)

Formal name: α-bicyclo[2.2.1]hept-5-en-2-yl-α-phenyl-1-piperidinepropanol, monohydrochloride

Synonyms:  NSC 170950|NSC 84989

Molecular weight: 347.9

CAS: 1235-82-1

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Neuroscience|Neurodegenerative Disorders|Parkinson’s Disease

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