radiolabeled

L-689560 是 N-甲基-D-天冬氨酸受体（NMDA）的有效拮抗剂，抑制 NMDA 甘氨酸结合位点。它用于研究 NMDA 受体在正常神经系统过程以及疾病中的作用，也广泛用作结合研究中的放射性标记配体，也。

D-Lysine(D-赖氨酸)是L-Lysine的 D 型异构体，可通过L-赖氨酸的化学消旋和微生物不对称降解制备。D-Lysine可减少放射性标记肽在肾脏的摄取，降低肾毒性。

JTE-013 是一种选择性S1P2拮抗剂。它抑制放射性标记的 S1P 与人和大鼠 S1P2的特异性结合，IC50分别为 17 nM 和 22 nM。

PSMA-D5 对PSMA展现出高结合亲和力，Ki值为0.21 nM。经过放射性标记后，它可用于PSMA示踪。PSMA-D5 ([68Ga] 标记) 包含DOTA螯合剂，可便捷地标记177Lu和225Ac等治疗性放射性核素。该化合物在22Rv1肿瘤中表现出显著的肿瘤摄取率，并具有优越的药代动力学特性。PSMA-D5 可用于合成或研究放射性核素偶联药物 (RDC)。

Martinostat是一种HDAC抑制剂，可放射性核素标记以用于体内中枢神经系统及主要外周器官中HDACs的定量成像。

AB-3PRGD2 是一种用于研究的放射性化合物，能够靶向整合素αvβ3。此化合物能够提高肿瘤摄取量并延长肿瘤中的滞留时间，显著增强对肿瘤生长的抑制效果。此外，AB-3PRGD2 可通过上调PD-L1的表达以及增加肿瘤浸润的CD8+T细胞来重塑肿瘤免疫微环境。

Dotanoc is a ligand to make gallium Ga 68-DOTANOC, which is a gallium Ga 68-radiolabeled analog of somatostatin.

Fet F-18 is an amino acid analog radiolabeled with fluorine F-18, a positron-emitting isotope, can be used as a tracer in positron emission tomography (PET).

Isoxaben (EL 107) 是一种细胞壁生物合成的特异性抑制剂，常作为除草剂使用，可抑制放射性标记的葡萄糖掺入酸不溶性细胞壁部分。

Heteroatom-substituted fatty acids have been observed to modulate the extension and desaturating of fatty acids, and to influence their distribution within phospholipids pools. 10-Thiastearic acid inhibits desaturation of radiolabeled stearate to oleate in rat hepatocytes and hepatoma cells by more than 80% at a concentration of 25 μM. This activity is associated with a hypolipidemic effect, making this 10-thiastearic acid a useful tool for evaluating new anti-obesity therapeutics.

2,3-dinor-11β-Prostaglandin F2α (2,3-dinor-11β-PGF2α) was recovered from the urine of both normal monkeys and humans when infused with radiolabeled PGD2, where it represented approximately 1% and 4% of the infused radiolabeled dose, respectively. 2,3-dinor-11β-PGF2α has also been recovered from the urine of mastocytosis patients, where it is excreted in large amounts. In human asthmatic patients, 2,3-dinor-11β-PGF2α represents about 40% (as determined by GC/MS) of the immunoreactive 11β-PGF2α when measured using 's 11β-PGF2α EIA Kit . The excretion rate for 2,3-dinor-11β-PGF2α is approximately 200-250 ng/24 hours in a normal adult.

MK-6884, a positive allosteric modulator (PAM) of M4 muscarinic receptors, exhibits a high affinity (Ki = 0.19 nM). It is a valuable compound for the investigation of neurodegenerative diseases. Additionally, MK-6884 can be efficiently radiolabeled with carbon-11, enabling its use as a PET imaging agent.

CCR4 antagonist 3-1 是一种具有较低活性的趋化因子受体 4 (CCR4) 拮抗剂，对 [125I]TARC (胸腺和活化调节趋化因子) 具有抑制作用，IC50 值为 1.7 μM。CCR4 antagonist 3-1 对放射标记的[125I]TARC和巨噬细胞来源的趋化因子(MDC) 与 CEM 细胞表面的CCR4 受体的结合有抑制作用， 并对 TARC 介导的 CEM 细胞的体外迁移有抑制作用，IC50 值为 6.4 μM。

THK-5105为芳基喹啉衍生物，具备与tau原纤维高度结合的亲和力。它对tau蛋白聚集体及含tau的阿尔茨海默病(AD)脑匀浆显示出显著的结合能力。18F-THK-5105展现出作为tau成像PET探针的潜能。

Iobenguane I 131 is a guanidine analog with specific affinity for tissues of the sympathetic nervous system and related tumors. The radiolabeled forms are used as antineoplastic agents and radioactive imaging agents. MIBG serves as a neuron-blocking agent which has a strong affinity for, and retention in, the adrenal medulla and also inhibits ADP-ribosyltransferase.

Cornigerine is a natural product analog of colchicine produced by Colchicum cornigerum that inhibited tubulin polymerization both with and without microtubule-associated proteins, inhibited the binding of radiolabeled colchicine to tubulin, and stimulated tubulin-dependent GTP hydrolysis.

Icapamespib, also known as PU-HZ 151, is a heat shock protein 90 (HSP90) inhibitor. PU-HZ151 showed EC50 of 5 nM in the FP assay as compared to 11 nM for PU-H71 and a logD of 2.37 as compared to 1.21 for PU-H71. PU-HZ151 and radiolabeled PU-HZ151 showed selectivity for epichaperomes over the individual chaperome members. Icapamespib demonstrated the ability to productively engage the target in cells, mice, and humans.

Asem F-18 is a radiolabeled antagonist for imaging the α7-nicotinic acetylcholine receptor with PET .

BMY-42393 is orally active and selective platelet aggregation inhibitor. BMY-42393 is also a prostacyclin partial agonist that inhibited ADP, collagen and thrombin-induced platelet aggregation (IC50 range 0.3 - 2.0 microM). BMY-42393 stimulated platelet adenylate cyclase activity (EC50 = 25 nM). Platelets treated with BMY 42393 showed an elevation of cAMP levels and activation of cAMP-dependent protein kinase. BMY 42393 also inhibited thrombin-induced elevation of intracellular free calcium. BMY 42393 competed for radiolabeled iloprost and PGE1 binding to platelet membranes (IC50; 170 nM and 130 nM, respectively).

Gemcitabine triphosphate (dFdCTP) 是 Gemcitabine 在细胞内的两种核苷代谢产物的一种。另一种是活性二磷酸 (dFdDTP)。Gemcitabine triphosphate 能够作为放射性标记探针成像研究的标准物，用于识别对 Gemcitabine 的肿瘤，并评估 Gemcitabine 被细胞摄取和保留性质。

ω-Conotoxin MVIIC TFA是具有26个残基的多肽和神经毒素，通过高亲和力结合电压敏感的神经元Ca ++ 通道（VGCC），优先阻断P型和q型Ca ++ 电流，可进行放射性标记并用于免疫沉淀测定。

WL12是一种专门针对程序性死亡配体1 (PD-L1)的结合肽，可通过多种放射性核素标记，生成放射性示踪剂，用于评估肿瘤中PD-L1的表达情况。

Rosopatamab（罗索帕妥单抗）是一种人源化单克隆抗体，靶向前列腺特异性膜抗原（PSMA），主要用于前列腺癌的研究和治疗。它可以通过双功能螯合剂 DOTA-NHS 酯与放射性同位素（如 177Lu）结合，形成放射性核素偶联药物（RDC），用于靶向治疗前列腺癌。

DOTA-JR11为SSTR2生长抑素受体拮抗剂，能经68Ga标记，应用于神经内分泌肿瘤（NETs）配对成像研究。