An α1-AR antagonist
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Nicergoline

Item No. 31573

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(8β)-10-methoxy-1,6-dimethyl-ergoline-8-methanol, 8-(5-bromo-3-pyridinecarboxylate)
CAS Number
27848-84-6
Synonyms
  • FI-6714
  • Nicotergoline
  • NSC 150531
  • TA-079
Molecular Formula
C24H26BrN3O3
Formula Weight
484.4
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlDMSO:PBS (pH 7.2) (1:9): 0.1 mg/mlEthanol: 10 mg/ml
λmax
227 nm
SMILES
CO[C@@]12C3=CC=CC4=C3C(C[C@@]1([H])N(C[C@@H](C2)COC(C5=CN=CC(Br)=C5)=O)C)=CN4C
InChi Code
InChI=1S/C24H26BrN3O3/c1-27-13-17-8-21-24(30-3,19-5-4-6-20(27)22(17)19)9-15(12-28(21)2)14-31-23(29)16-7-18(25)11-26-10-16/h4-7,10-11,13,15,21H,8-9,12,14H2,1-3H3/t15-,21-,24+/m1/s1
InChi Key
YSEXMKHXIOCEJA-FVFQAYNVSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    100 mg

    $42

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    250 mg

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    500 mg

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    1 g

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    Product Description

    Nicergoline is an antagonist of α1-adrenergic receptors (α1-ARs).1 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.2 It also increases corneal NGF levels and accelerates corneal wound healing in a rat model of ocular injury.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Alvarez-Guerra, M., Bertholom, N., and Garay, R.P. Selective blockade by nicergoline of vascular responses elicited by stimulation of alpha1A‐adrenoceptor subtype in the rat. Fundam. Clin. Pharmacol. 13(1), 50-58 (1999).

    2. Asai, S., Zhao, H., Yamashita, A., et al. Nicergoline enhances glutamate re-uptake and protects against brain damage in rat global brain ischemia. Eur. J. Pharmacol. 383(3), 267-274 (1999).

    3. Kim, S.-Y., Choi, J.-S., and Joo, C.-K. Effects of nicergoline on corneal epithelial wound healing in rat eyes. Invest. Ophthalmol. Vis. Sci. 50(2), 621-625 (2009).