Nicergoline

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Nicergoline

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Catalog Number	PR27848846
CAS	27848-84-6
Description	An ergot derivative that has been used as a cerebral vasodilator and in peripheral vascular disease. It has been suggested to ameliorate cognitive deficits in cerebrovascular disease.
Synonyms	Nimergoline; ergobel; Nicotergoline; Sermion; cergodum; duracebrol
IUPAC Name	[(6aR,9R,10aS)-10a-methoxy-4,7-dimethyl-6a,8,9,10-tetrahydro-6H-indolo[4,3-fg]quinolin-9-yl]methyl 5-bromopyridine-3-carboxylate
Molecular Weight	484.4
Molecular Formula	C24H26BrN3O3
InChI	YSEXMKHXIOCEJA-FVFQAYNVSA-N
InChI Key	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
Associated Therapies	Peripheral vasodilatation
Documentation/Certification	Tech Pack
Drug Categories	Adrenergic Agents; Adrenergic alpha-1 Receptor Antagonists; Adrenergic alpha-Antagonists; Adrenergic Antagonists; Agents that produce hypertension; Alkaloids; Cardiovascular Agents; Central Nervous System Agents; Cytochrome P-450 CYP2D6 Substrates; Cytochrome P-450 Substrates; Ergolines; Ergot Alkaloids and Derivatives; Heterocyclic Compounds, Fused-Ring; Neurotransmitter Agents; Nootropic Agents; Peripheral Vasodilators; Vasodilating Agents
Drug Interactions	Abatacept-The metabolism of Nicergoline can be increased when combined with Abatacept. Abiraterone-The metabolism of Nicergoline can be decreased when combined with Abiraterone. Acebutolol-Acebutolol may increase the vasoconstricting activities of Nicergoline. Aceclofenac-The risk or severity of hypertension can be increased when Nicergoline is combined with Aceclofenac. Acemetacin-The risk or severity of hypertension can be increased when Nicergoline is combined with Acemetacin.
Isomeric SMILES	CN1C[C@@H](C[C@]2([C@H]1CC3=CN(C4=CC=CC2=C34)C)OC)COC(=O)C5=CC(=CN=C5)Br
Standard	ICH
Type	Small Molecule
Therapeutic Category	Dementia

Pharmacology

Indications

Nicergoline is primarily indicated for the management of several conditions related to vascular health. These include senile dementia and migraines of vascular origin. Additionally, it is utilized in treating transient ischemia, platelet hyper-aggregability, and macular degeneration. The use of Nicergoline in these conditions highlights its role in addressing issues related to blood flow and vascular function.

Pharmacodynamics

As a potent vasodilator, Nicergoline plays a critical role in enhancing cerebral blood flow. It achieves this by reducing vascular resistance, increasing arterial flow, and promoting the utilization of oxygen and glucose in the brain. Moreover, Nicergoline contributes to improved blood circulation not only in the brain but also in the lungs and limbs. One of its significant actions includes the inhibition of blood platelet aggregation, which aids in preventing clot formation and thus, supports overall vascular health.

Mechanism of Action

Nicergoline functions by inhibiting the postsynaptic alpha(1)-adrenoceptors located on the vascular smooth muscle. This inhibition counteracts the vasoconstrictor effects of both circulating and locally released catecholamines, such as epinephrine and norepinephrine, leading to peripheral vasodilation. Consequently, Nicergoline facilitates increased vascular circulation, particularly within the brain, and enhances the transmission of nerve signals. This improved neural communication involves the secretion of acetylcholine as a neurotransmitter.

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