TEMECHINE - CAS 30015-57-7

a neuronal nicotinic AChR antagonist. Potent ganglioblocker. Hypotensive. Good penetration of biological membranes. Rigid bicyclic analog of Pempidine. Non-quaternary analog of Quirestine.


Quinicludine derivative,11H21N .HBr–>, synthetic.

For comparative information see the attached 2 tables.
Cell permeant central nicotinic acetylcholine receptor blocker without action on skeleton muscle innervation. Quinuclidine analog of Pempidine, non-quaternary analog of Quirestine. Hypotensive, selectively blocks autonomic ganglia, the adrenal medulla, carotid glomerules.

Three-fold more active than Pempidine, wide therapeutic range [1]. Slows down neuronal pre- and post ganglionar transmission: dilates peripheral vessels and bronchi, arterial pressure and pressor reaction drop. Suppresses gland secretion. Sedative.

Good penetration of biological membranes.

Blocks superior cervical sympathetic ganglion (electrical stimulation of cats nictiating membrane): ED50 = 17 �g/kg , Pempidine 54 �g/kg.

Blocks autonomic ganglion ( vagus electrical stimulation): depressor reaction suppression – 50 �g /kg 40%, 500 �g/kg 100%. After 100% nicotinic blockade with 500 �g /kg, cardiac system still reacts to muscarinic action of ACh (i.v.).


Catalog Number: T000142

CAS Number: 30015-57-7

PubChem Substance ID:355427968

Molecular Formula: C11H22BrN

Molecular Weight:248.208

Purity: ≥95%

* For research use only. Not for human or veterinary use.

Synonym

Synonyms2,2,6,6-tetramethylquinicludine hydrobromide.

Property

Molecular Formula: C11H22BrN
Molecular Weight248.208
Solubilitywater, ethanol (1 g in 10 ml).
Purity≥95%
Storagestore at room temperature. Solution for use: dissolve in water: 10-3M (2 mg in 8.06 ml), stable for 1-2 days at 20C.

Computed Descriptor

IUPAC Name2,2,6,6-tetramethyl-1-azabicyclo[2.2.2]octane;hydrobromide
InChIInChI=1S/C11H21N.BrH/c1-10(2)7-9-5-6-12(10)11(3,4)8-9;/h9H,5-8H2,1-4H3;1H
InChIKeyPKYZWCLYWCKYNX-UHFFFAOYSA-N
SMILESCC1(CC2CCN1C(C2)(C)C)C.Br