跳转至内容

很抱歉,目前系统维护中。在此期间,网站下单功能无法使用。给您带来不便,深表歉意。如需其他帮助,请联系客户联络中心:400 620 3333。

Merck
CN
  • (11)C-CUMI-101, a PET radioligand, behaves as a serotonin 1A receptor antagonist and also binds to α(1) adrenoceptors in brain.

(11)C-CUMI-101, a PET radioligand, behaves as a serotonin 1A receptor antagonist and also binds to α(1) adrenoceptors in brain.

Journal of nuclear medicine : official publication, Society of Nuclear Medicine (2014-01-05)
Stal Saurav Shrestha, Jeih-San Liow, Shuiyu Lu, Kimberly Jenko, Robert L Gladding, Per Svenningsson, Cheryl L Morse, Sami S Zoghbi, Victor W Pike, Robert B Innis
摘要

The PET radioligand (11)C-CUMI-101 was previously suggested as a putative agonist radioligand for the serotonin 1A (5-hydroxytryptamine 1A [5-HT1A]) receptor in recombinant cells expressing human 5-HT1A receptor. However, a recent study showed that CUMI-101 behaved as a potent 5-HT1A receptor antagonist in rat brain. CUMI-101 also has moderate affinity (Ki = 6.75 nM) for α1 adrenoceptors measured in vitro. The current study examined the functional properties and selectivity of CUMI-101, both in vitro and in vivo. The functional assay was performed using (35)S-GTPγS (GTP is guanosine triphosphate) in primate brains. The cross-reactivity of CUMI-101 with α1 adrenoceptors was performed using in vitro radioligand binding studies in rat, monkey, and human brains as well as in vivo PET imaging in mouse, rat, and monkey brains. CUMI-101 did not stimulate (35)S-GTPγS binding in primate brain, in contrast to 8-OH-DPAT, a potent 5-HT1A receptor agonist. Instead, CUMI-101 behaved as a potent 5-HT1A receptor antagonist by dose-dependently inhibiting 8-OH-DPAT-stimulated (35)S-GTPγS binding. Both in vitro and in vivo studies showed that CUMI-101 had significant α1 adrenoceptor cross-reactivity. On average, across all 3 species examined, cross-reactivity was highest in the thalamus (>45%) and lowest in the neocortex and cerebellum (<10%). PET imaging further confirmed that only preblocking with WAY-100635 plus prazosin decreased (11)C-CUMI-101 brain uptake to that of self-block. CUMI-101 behaves as a 5-HT1A receptor antagonist in primate brain, with significant, regional-dependent α1 adrenoceptor cross-reactivity, limiting its potential use as a PET radioligand in humans.

材料
货号
品牌
产品描述

Sigma-Aldrich
哌唑嗪 盐酸盐, ≥99.0% (HPLC)
登录查看公司和协议定价
货号包装规格是否有货价格数量
10 mg
国内现货,预计发货时间 April 07, 2025
详情...
CN¥375.91
25 mg
国内现货,预计发货时间 April 07, 2025
详情...
CN¥750.49
100 mg
国内现货,预计发货时间 April 07, 2025
详情...
CN¥2,144.28
250 mg
国内现货,预计发货时间 April 07, 2025
详情...
CN¥2,560.22
500 mg
国内现货,预计发货时间 April 07, 2025
详情...
CN¥4,670.90
1 g
国内现货,预计发货时间 April 07, 2025
详情...
CN¥9,529.50