SR 48692は、高親和性かつ経口でバイオアベイラブルであり、選択的な非ペプチドNT1ニューロテンシン受容体アンタゴニストであり、HT-29ヒト大腸癌細胞株においてニューロテンシン誘発カルシウムの動員（pA2 8.13）をアンタゴナイズし、前頭前皮質においてニューロテンシンのGABA上昇能をブロックします。
SR 48692は、高親和性かつ経口でバイオアベイラブルであり、選択的な非ペプチドNT1ニューロテンシン受容体アンタゴニストです。
特徴および利点
この化合物はHandbook of Receptor Classification and Signal Transduction（受容体分類およびシグナル変換ハンドブック）のNeurotensin Receptorsのページに取り上げられています。ハンドブックのその他のページをご覧になるには、ここをクリックしてください。
Tridecapeptide neurotensin (NT) acts as a neurotransmitter and/or neuromodulator and plays a role in learning and reinforcement. The central nucleus of amygdala (CeA), which is relatively rich in NT and neurotensin-1 receptors (NTS1), participates in the regulation of memory and
In a search for nonpeptide agonists for the neurotensin receptor (NTR1), we replaced the adamantyl amino acid moiety found in the antagonist SR48692 (1a) with leucine and related alpha-alkylamino acids found in peptide agonists. When tested in a calcium mobilization
Psychostimulant-induced locomotor sensitization has been related to changes within the mesolimbic dopamine system and has been suggested to be useful to study mechanisms underlying drug craving. Neurotensin is a neuropeptide co-localized with dopamine in the mesolimbic system. The response to
The European journal of neuroscience, 24(10), 2789-2800 (2006-11-23)
Several lines of evidence suggest a close association between dopamine (DA) and neurotensin (NT) systems in the CNS. Indeed, in the rodent brain, abundant NT-containing fibres are found in DA-rich areas such as the ventral tegmental area and substantia nigra.
In the central nervous system neurotensin (NT) acts as a neurotransmitter and neuromodulator. It was shown that NT has positive reinforcing effects after its direct microinjection into the ventral tegmental area. The central nucleus of amygdala (CeA), part of the
