Bioorganic & Medicinal Chemistry Letters 2001-02-12

Nipecotic and iso-nipecotic amides as potent and selective somatostatin subtype-2 receptor agonists.

C Zhou, L Guo, G Morriello, A Pasternak, Y Pan, S P Rohrer, E T Birzin, S E Huskey, T Jacks, K D Schleim, K Cheng, J M Schaeffer, A A Patchett, L Yang

Index: Bioorg. Med. Chem. Lett. 11(3) , 415-7, (2001)

Full Text: HTML

Abstract

N-Substituted nipecotic and iso-nipecotic amides of beta-methylTrpLys tert-butyl ester were found to be novel, selective and potent agonists of the somatostatin subtype-2 receptor in vitro. For example iso-nipecotic amide 8a showed high hsst2 binding affinity (Ki = 0.5 nM) and good selectivity (h5/h2 = 832).

Related Compounds

  • Nipecotamide

Related Articles:

Effects of sodium n-dipropylacetate, muscimol hydrobromide and (R,S) nipecotic acid amide on isolation-induced aggressive behavior in mice.

1980-01-01

[Psychopharmacology 70(3) , 287-90, (1980)]

Gabaergic modulation of mouse-killing in the rat.

1984-01-01

[Psychopharmacology 83(4) , 367-72, (1984)]

Relationships between the chemical constitution of carbamoylpiperidines and related compounds, and their inhibition of ADP-induced human blood platelet aggregation.

1981-01-01

[Thromb. Res. 22(5-6) , 665-80, (1981)]

More Articles...