An α1-AR antagonist; binds to α1-ARs in rat brain membranes (Ki = 12.5 nM); inhibits α1-AR agonist-induced contractions in endothelium-denuded isolated rat aortic rings and perfused mesenteric vascular beds (pA2s = 8.6 and 11.1

Nicergoline – 250 mg

Brand:
Cayman
CAS:
27848-84-6
Storage:
-20
UN-No:
Non-Hazardous - /

Nicergoline is an antagonist of α1-adrenergic receptors (α1-ARs).{59212} It binds to α1-ARs in rat brain membranes (Ki = 12.5 nM) and inhibits α1-AR agonist-induced contractions in endothelium-denuded isolated rat aortic rings and perfused mesenteric vascular beds (pA2s = 8.6 and 11.1, respectively). In vivo, nicergoline (0.5 µg/kg per minute, i.v.) inhibits pressor responses induced by the α1-AR agonist cirazoline (Item No. 21791) in pithed rats. Nicergoline (32 mg/kg) improves post-ischemic glutamate uptake and reduces neuronal cell death and mortality in a rat model of global brain ischemia induced by mild hyperthermia.{59213} It also increases corneal NGF levels and accelerates corneal wound healing in a rat model of ocular injury.{59214}  

 

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Description

An α1-AR antagonist; binds to α1-ARs in rat brain membranes (Ki = 12.5 nM); inhibits α1-AR agonist-induced contractions in endothelium-denuded isolated rat aortic rings and perfused mesenteric vascular beds (pA2s = 8.6 and 11.1, respectively); inhibits cirazoline-induced pressor responses in rats at 0.5 µg/kg per minute, i.v.; improves postischemic glutamate uptake and reduces neuronal cell death and mortality in a rat model of global brain ischemia induced by mild hyperthermia at 32 mg/kg; increases corneal NGF levels and accelerates corneal wound healing in a rat model of ocular injury

Formal name: (8β)-10-methoxy-1,6-dimethyl-ergoline-8-methanol, 8-(5-bromo-3-pyridinecarboxylate)

Synonyms:  FI-6714|Nicotergoline|NSC 150531|TA-079

Molecular weight: 484.4

CAS: 27848-84-6

Purity: ≥98%

Formulation: A solid

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